cisatracurium ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
neuromuscular blocking agents with rigid structure 661 96946-42-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cisatracurium besylate
  • cisatracurium besilate
  • cisatracurium
  • Molecular weight: 929.16
  • Formula: C53H72N2O12
  • CLOGP: 3.30
  • LIPINSKI: 2
  • HAC: 14
  • HDO: 0
  • TPSA: 126.44
  • ALOGS: -7.63
  • ROTB: 26

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 0 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 8.50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.65 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 0.14 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 5.40 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.62 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 0.42 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Dec. 15, 1995 FDA ABBVIE

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Anaphylactic shock 348.63 44.29 97 2439 20058 50582530
Anaphylactic reaction 126.12 44.29 59 2477 53996 50548592
Hypotension 97.72 44.29 86 2450 235383 50367205
Bronchospasm 96.90 44.29 34 2502 14820 50587768
Mixed liver injury 94.67 44.29 24 2512 3427 50599161
Cardiac arrest 88.70 44.29 54 2482 83597 50518991
Circulatory collapse 76.56 44.29 31 2505 19969 50582619
Multiple organ dysfunction syndrome 73.35 44.29 40 2496 50297 50552291
Myoclonus 67.92 44.29 26 2510 14444 50588144
Cardiogenic shock 66.02 44.29 26 2510 15573 50587015
Bradycardia 59.16 44.29 38 2498 64388 50538200
Post procedural complication 49.62 44.29 21 2515 15083 50587505
Sinus tachycardia 45.67 44.29 22 2514 21332 50581256

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Anaphylactic shock 262.08 31.32 83 2884 13253 29558307
Hypertransaminasaemia 125.59 31.32 35 2932 3571 29567989
Anaphylactic reaction 121.78 31.32 58 2909 27515 29544045
Hyperthermia malignant 113.79 31.32 28 2939 1756 29569804
Rhabdomyolysis 81.46 31.32 59 2908 60749 29510811
Bronchospasm 70.81 31.32 29 2938 9580 29561980
Toxic epidermal necrolysis 61.70 31.32 32 2935 18121 29553439
Shock 59.47 31.32 33 2934 21371 29550189
Hypotension 57.41 31.32 83 2884 194271 29377289
Drug reaction with eosinophilia and systemic symptoms 56.28 31.32 35 2932 27957 29543603
Klebsiella infection 50.14 31.32 21 2946 7328 29564232
Acute respiratory distress syndrome 49.47 31.32 30 2937 22905 29548655
Serotonin syndrome 48.64 31.32 27 2940 17485 29554075
Septic shock 42.43 31.32 41 2926 62519 29509041
Hypoxia 41.81 31.32 36 2931 47343 29524217
Vasoplegia syndrome 40.66 31.32 12 2955 1496 29570064
Pseudomonal sepsis 40.36 31.32 14 2953 2928 29568632
Haemodynamic instability 38.68 31.32 18 2949 8055 29563505
COVID-19 37.23 31.32 30 2937 35984 29535576
Cardiac arrest 36.69 31.32 44 2923 85547 29486013
Circulatory collapse 36.63 31.32 23 2944 18650 29552910
Metabolic acidosis 31.96 31.32 28 2939 37634 29533926
Burkholderia test positive 31.59 31.32 9 2958 990 29570570

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Anaphylactic shock 577.90 31.08 176 5147 30152 64463257
Anaphylactic reaction 231.94 31.08 113 5210 68551 64424858
Bronchospasm 159.94 31.08 62 5261 21620 64471789
Hypotension 131.70 31.08 159 5164 380815 64112594
Hyperthermia malignant 130.24 31.08 32 5291 2427 64490982
Hypertransaminasaemia 112.50 31.08 36 5287 7155 64486254
Cardiac arrest 103.38 31.08 92 5231 153972 64339437
Circulatory collapse 94.52 31.08 49 5274 33683 64459726
Shock 86.00 31.08 48 5275 38192 64455217
Multiple organ dysfunction syndrome 83.16 31.08 68 5255 101345 64392064
Mixed liver injury 75.81 31.08 25 5298 5456 64487953
Rhabdomyolysis 74.13 31.08 61 5262 91665 64401744
Acute respiratory distress syndrome 69.31 31.08 42 5281 38893 64454516
Toxic epidermal necrolysis 68.51 31.08 41 5282 37125 64456284
Hypoxia 65.79 31.08 56 5267 88093 64405316
Bradycardia 53.58 31.08 57 5266 118162 64375247
Cardiogenic shock 50.16 31.08 32 5291 32395 64461014
Drug reaction with eosinophilia and systemic symptoms 47.87 31.08 38 5285 54179 64439230
Tachycardia 47.43 31.08 60 5263 149519 64343890
Septic shock 46.29 31.08 50 5273 105387 64388022
Haemodynamic instability 45.62 31.08 23 5300 14889 64478520
Cyanosis 44.90 31.08 26 5297 22129 64471280
Myoclonus 44.44 31.08 27 5296 25091 64468318
Vasoplegia syndrome 43.87 31.08 14 5309 2753 64490656
Ventricular fibrillation 43.12 31.08 26 5297 23834 64469575
Klebsiella infection 42.14 31.08 21 5302 13260 64480149
Metabolic acidosis 39.02 31.08 38 5285 70920 64422489
Hepatocellular injury 38.42 31.08 31 5292 45204 64448205
Serotonin syndrome 37.85 31.08 29 5294 39253 64454156
Fatigue 35.72 31.08 9 5314 748721 63744688
Blood pressure decreased 34.57 31.08 39 5284 86160 64407249
Diarrhoea 33.87 31.08 9 5314 722695 63770714
Nausea 32.87 31.08 12 5311 785788 63707621
Sinus tachycardia 31.53 31.08 24 5299 32164 64461245

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC M03AC11 MUSCULO-SKELETAL SYSTEM
MUSCLE RELAXANTS
MUSCLE RELAXANTS, PERIPHERALLY ACTING AGENTS
Other quaternary ammonium compounds
CHEBI has role CHEBI:48878 nicotinic antagonists
CHEBI has role CHEBI:51371 muscle relaxants
MeSH PA D009465 Neuromuscular Agents
MeSH PA D009466 Neuromuscular Blocking Agents
MeSH PA D018373 Peripheral Nervous System Agents
FDA EPC N0000175720 Nondepolarizing Neuromuscular Blocker
FDA PE N0000175732 Neuromuscular Nondepolarizing Blockade

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Muscle relaxation, function indication 11977004
General anesthesia indication 50697003
Skeletal Muscle Relaxation for Endotracheal Intubation indication
Disorder of lung contraindication 19829001 DOID:850
Myasthenia gravis contraindication 91637004 DOID:437
Disorder of electrolytes contraindication 237840007
Malignant hyperthermia contraindication 405501007




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Acetylcholine receptor Ion channel ANTAGONIST IC50 8 WOMBAT-PK CHEMBL

External reference:

IDSource
4020957 VUID
N0000148433 NUI
D00759 KEGG_DRUG
136561 RXNORM
4020957 VANDF
4024019 VANDF
C1096766 UMLSCUI
CHEBI:3721 CHEBI
CHEMBL1201248 ChEMBL_ID
CHEMBL1200641 ChEMBL_ID
DB00565 DRUGBANK_ID
C101584 MESH_SUPPLEMENTAL_RECORD_UI
QX62KLI41N UNII
62887 PUBCHEM_CID
192613 MMSL
36562 MMSL
4455 MMSL
d03875 MMSL
005186 NDDF
005213 NDDF
108452005 SNOMEDCT_US
108453000 SNOMEDCT_US
372495006 SNOMEDCT_US
7389 INN_ID
96946-41-7 SECONDARY_CAS_RN

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Nimbex HUMAN PRESCRIPTION DRUG LABEL 1 0074-4378 INJECTION 2 mg INTRAVENOUS NDA 27 sections
Nimbex HUMAN PRESCRIPTION DRUG LABEL 1 0074-4380 INJECTION 2 mg INTRAVENOUS NDA 27 sections
Nimbex HUMAN PRESCRIPTION DRUG LABEL 1 0074-4382 INJECTION 10 mg INTRAVENOUS NDA 27 sections
Cisatracurium Besylate HUMAN PRESCRIPTION DRUG LABEL 1 0409-1098 INJECTION, SOLUTION 2 mg INTRAVENOUS ANDA 28 sections
Cisatracurium Besylate HUMAN PRESCRIPTION DRUG LABEL 1 0409-1098 INJECTION, SOLUTION 2 mg INTRAVENOUS ANDA 28 sections
Cisatracurium Besylate HUMAN PRESCRIPTION DRUG LABEL 1 0409-1103 INJECTION, SOLUTION 10 mg INTRAVENOUS ANDA 28 sections
Cisatracurium Besylate HUMAN PRESCRIPTION DRUG LABEL 1 0409-1103 INJECTION, SOLUTION 10 mg INTRAVENOUS ANDA 28 sections
Cisatracurium Besylate HUMAN PRESCRIPTION DRUG LABEL 1 0409-1208 INJECTION, SOLUTION 2 mg INTRAVENOUS ANDA 28 sections
Cisatracurium Besylate HUMAN PRESCRIPTION DRUG LABEL 1 0409-1208 INJECTION, SOLUTION 2 mg INTRAVENOUS ANDA 28 sections
Cisatracurium Besylate HUMAN PRESCRIPTION DRUG LABEL 1 0409-3670 INJECTION, SOLUTION 10 mg INTRAVENOUS ANDA 30 sections
Cisatracurium Besylate HUMAN PRESCRIPTION DRUG LABEL 1 0409-5547 INJECTION, SOLUTION 2 mg INTRAVENOUS ANDA 30 sections
Cisatracurium Besylate HUMAN PRESCRIPTION DRUG LABEL 1 0409-7083 INJECTION, SOLUTION 2 mg INTRAVENOUS ANDA 30 sections
Cisatracurium Besylate HUMAN PRESCRIPTION DRUG LABEL 1 0703-2033 INJECTION 10 mg INTRAVENOUS ANDA 25 sections
Cisatracurium Besylate HUMAN PRESCRIPTION DRUG LABEL 1 0703-2045 INJECTION 200 mg INTRAVENOUS ANDA 25 sections
Cisatracurium Besylate HUMAN PRESCRIPTION DRUG LABEL 1 0703-2056 INJECTION 20 mg INTRAVENOUS ANDA 25 sections
cisatracurium besylate HUMAN PRESCRIPTION DRUG LABEL 1 0781-3150 INJECTION 2 mg INTRAVENOUS ANDA 25 sections
cisatracurium besylate HUMAN PRESCRIPTION DRUG LABEL 1 0781-3152 INJECTION 2 mg INTRAVENOUS ANDA 25 sections
cisatracurium besylate HUMAN PRESCRIPTION DRUG LABEL 1 0781-3153 INJECTION 10 mg INTRAVENOUS ANDA 25 sections
Cisatracurium Besylate Human Prescription Drug Label 1 24584-1110 INJECTION 2 mg INTRAVENOUS ANDA 26 sections
Cisatracurium Besylate Human Prescription Drug Label 1 24584-1111 INJECTION 2 mg INTRAVENOUS ANDA 26 sections
Cisatracurium Besylate Human Prescription Drug Label 1 24584-1112 INJECTION 2 mg INTRAVENOUS ANDA 26 sections
Cisatracurium Besylate HUMAN PRESCRIPTION DRUG LABEL 1 25021-668 INJECTION, SOLUTION 2 mg INTRAVENOUS ANDA 26 sections
Cisatracurium Besylate HUMAN PRESCRIPTION DRUG LABEL 1 25021-669 INJECTION, SOLUTION 10 mg INTRAVENOUS ANDA 26 sections
Cisatracurium Besylate HUMAN PRESCRIPTION DRUG LABEL 1 25021-670 INJECTION, SOLUTION 2 mg INTRAVENOUS ANDA 26 sections
Cisatracurium besylate Human Prescription Drug Label 1 55150-284 INJECTION 10 mg INTRAVENOUS ANDA 25 sections
Cisatracurium Besylate Human Prescription Drug Label 1 55150-286 INJECTION 20 mg INTRAVENOUS ANDA 25 sections
Cisatracurium HUMAN PRESCRIPTION DRUG LABEL 1 63323-416 INJECTION, SOLUTION 2 mg INTRAVENOUS ANDA 12 sections
Cisatracurium HUMAN PRESCRIPTION DRUG LABEL 1 63323-417 INJECTION, SOLUTION 2 mg INTRAVENOUS ANDA 12 sections
Cisatracurium HUMAN PRESCRIPTION DRUG LABEL 1 63323-418 INJECTION, SOLUTION 10 mg INTRAVENOUS ANDA 12 sections
Cisatracurium Besylate HUMAN PRESCRIPTION DRUG LABEL 1 70069-141 INJECTION 2 mg INTRAVENOUS ANDA 24 sections