sufentanil Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
opioid receptor agonists, analgesics, fentanyl derivatives 2491 56030-54-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • sulfentanyl
  • sulfentanil
  • sulfentanil citrate
  • sufentanil
  • sufentanil citrate
An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent.
  • Molecular weight: 386.55
  • Formula: C22H30N2O2S
  • CLOGP: 3.59
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 32.78
  • ALOGS: -4.51
  • ROTB: 8

Drug dosage:

None

Approvals:

DateAgencyCompanyOrphan
May 4, 1984 FDA AKORN

FDA Adverse Event Reporting System

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 541.34 63.86 101 643 5638 3379477
Hypotension 377.04 63.86 113 631 49401 3335714
Bronchospasm 257.48 63.86 52 692 4242 3380873
Exposure during pregnancy 247.73 63.86 72 672 27491 3357624
Circulatory collapse 126.50 63.86 31 713 6018 3379097
Cognitive disorder 118.38 63.86 31 713 7843 3377272
Drug ineffective 100.34 63.86 56 688 116034 3269081
Shock 93.17 63.86 25 719 6912 3378203
Bradycardia 91.34 63.86 30 714 16639 3368476
Cardiac arrest 91.33 63.86 34 710 27285 3357830
Tachycardia 85.14 63.86 31 713 23340 3361775
Foetal growth restriction 67.74 63.86 15 729 1854 3383261
Hyperthermia malignant 66.05 63.86 12 732 542 3384573
Hepatocellular injury 64.46 63.86 17 727 4378 3380737

Pharmacologic Action:

SourceCodeDescription
ATC N01AH03 NERVOUS SYSTEM
ANESTHETICS
ANESTHETICS, GENERAL
Opioid anesthetics
MeSH PA D000759 Adjuvants, Anesthesia
MeSH PA D000700 Analgesics
MeSH PA D000701 Analgesics, Opioid
MeSH PA D000777 Anesthetics
MeSH PA D018681 Anesthetics, General
MeSH PA D018686 Anesthetics, Intravenous
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D009294 Narcotics
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents
CHEBI has role CHEBI:35482 opioid analgesic
CHEBI has role CHEBI:55322 mu-opioid receptor agonist
CHEBI has role CHEBI:60807 anaesthesia adjuvant
CHEBI has role CHEBI:38877 intravenous anaesthetic
FDA MoA N0000175684 Full Opioid Agonists
FDA EPC N0000175690 Opioid Agonist

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
General anesthesia indication 50697003
Postoperative pain indication 213299007
Asthenia contraindication 13791008
Chronic disease of respiratory system contraindication 17097001
Decreased cardiac function contraindication 43650005
Bradycardia contraindication 48867003
Injury of head contraindication 82271004
Kidney disease contraindication 90708001 DOID:2527
Disease of liver contraindication 235856003 DOID:409

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.37 Basic

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
Mu-type opioid receptor GPCR AGONIST EC50 8.13 WOMBAT-PK CHEMBL
Delta-type opioid receptor GPCR Ki 7.30 PDSP
Kappa-type opioid receptor GPCR EC50 6.70 WOMBAT-PK
Opioid receptor GPCR Ki 10.70 CHEMBL
Mu-type opioid receptor GPCR Ki 9.66 CHEMBL

External reference:

IDSource
3534 IUPHAR_LIGAND_ID
4019936 VUID
N0000148021 NUI
C0143993 UMLSCUI
D00845 KEGG_DRUG
CHEMBL658 ChEMBL_ID
DB00708 DRUGBANK_ID
4019936 VANDF
N0000007169 NDFRT
N0000148021 NDFRT
56795 RXNORM
d00378 MMSL
004630 NDDF
49998007 SNOMEDCT_US
370275005 SNOMEDCT_US
AFE2YW0IIZ UNII
4048 INN_ID
41693 PUBCHEM_CID
CHEMBL1201163 ChEMBL_ID
60561-17-3 SECONDARY_CAS_RN
D017409 MESH_DESCRIPTOR_UI
CHEBI:9316 CHEBI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Sufentanil Citrate HUMAN PRESCRIPTION DRUG LABEL 1 0409-3380 INJECTION, SOLUTION 50 ug EPIDURAL ANDA 19 sections
Sufentanil Citrate HUMAN PRESCRIPTION DRUG LABEL 1 0409-3382 INJECTION, SOLUTION 50 ug EPIDURAL ANDA 19 sections
Sufentanil Citrate HUMAN PRESCRIPTION DRUG LABEL 1 0641-6110 INJECTION 0.05 mg EPIDURAL ANDA 13 sections
Sufentanil Citrate HUMAN PRESCRIPTION DRUG LABEL 1 0641-6111 INJECTION 0.05 mg EPIDURAL ANDA 13 sections
Sufentanil Citrate HUMAN PRESCRIPTION DRUG LABEL 1 0641-6112 INJECTION 0.05 mg EPIDURAL ANDA 13 sections
Sufentanil Citrate HUMAN PRESCRIPTION DRUG LABEL 1 17478-050 INJECTION 50 ug INTRAVENOUS NDA 18 sections