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
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 |
---|---|---|
Recent advances in myorelaxant therapy. | 2001 |
|
Malignant hyperthermia in a patient with Graves' disease during subtotal thyroidectomy. | 2001 Apr |
|
Ultra-fast-track anesthetic technique facilitates operating room extubation in patients undergoing off-pump coronary revascularization surgery. | 2001 Apr |
|
Effect of halothane on the cerebral circulation in young children: a hysteresis phenomenon. | 2001 Apr |
|
Overdistension in ventilated children. | 2001 Aug |
|
Small dose of prostaglandin E(1) increases cardiac output without altering blood volume. | 2001 Aug |
|
Safety and efficacy of rocuronium for controlled intubation with paralytics in the pediatric emergency department. | 2001 Aug |
|
A multicenter evaluation of the time-course of action of two doses of rapacuronium after early and late reversal with neostigmine. | 2001 Aug |
|
Unmasked residual neuromuscular block after administration of vecuronium for days. | 2001 Aug |
|
The laryngeal mask airway is effective (and probably safe) in selected healthy parturients for elective Cesarean section: a prospective study of 1067 cases. | 2001 Dec |
|
Pharmacokinetics and pharmacodynamics of vecuronium in children receiving phenytoin or carbamazepine for chronic anticonvulsant therapy. | 2001 Feb |
|
Comparison of no airway device, the Guedel-type airway and the Cuffed Oropharyngeal Airway with mask ventilation during manual in-line stabilization. | 2001 Feb |
|
[Prevention of postoperative nausea and vomiting in gynecologic surgery with 3 fixed doses of metoclopramide, droperidol or placebo]. | 2001 Feb |
|
Nicorandil accelerates recovery of neuromuscular block caused by vecuronium. | 2001 Jan |
|
[A case of ventricular tachycardia immediately after electroconvulsive therapy in a schinzophrenic patient]. | 2001 Jan |
|
[Pulmonary embolism during laparoscopic cholecystectomy detected by sudden decrease in end-tidal carbon dioxide pressure]. | 2001 Jan |
|
Vaginal physiological changes in a model of sexual arousal in anesthetized rats. | 2001 Jul |
|
Bispectral index monitoring in sevoflurane and remifentanil anesthesia. Analysis of drugs management and immediate recovery. | 2001 Jun |
|
Pediatric renal transplantation: anesthesia and perioperative complications. | 2001 Mar |
|
[Perioperative administration of bicarbonated solution to a patient with mitochondrial encephalomyopathy]. | 2001 Mar |
|
Cesarean section in a patient with syringomyelia. | 2001 May |
|
Severe bronchospasm and desaturation in a child associated with rapacuronium. | 2001 May |
|
Rapacuronium and bronchospasm. | 2001 May |
|
A case of awareness with sevoflurane and epidural anesthesia in ovarian tumorectomy. | 2001 May |
|
[Two pediatric cases of malignant hyperthermia caused by sevoflurane]. | 2001 Nov |
|
Severe bradycardia during epilepsy surgery. | 2001 Oct |
|
[Anesthesia for a patient with alcoholic heart disease and transient complete heart block]. | 2001 Oct |
|
[Anesthetic management of a patient with Dyggve-Melchior-Clausen syndrome]. | 2001 Oct |
|
Systemic spread of vecuronium following use in peribulbar regional anaesthesia. | 2001 Oct |
|
Reexamined: the recommended endotracheal intubating dose for nondepolarizing neuromuscular blockers of rapid onset. | 2001 Oct |
|
[The effects of the fat component of propofol solution of ketogenesis during propofol anesthesia]. | 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.
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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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ACTIVE MOIETY
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