remifentanil indications/contra

Stem definitionDrug idCAS RN
opioid receptor agonists, analgesics, fentanyl derivatives 2363 132875-61-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • remifentanil
  • remifentanyl
  • ramifentanyl
  • remifentanil hydrochloride
  • remifentanil HCl
Remifentanil is a mu-opioid agonist with rapid onset and peak effect, and short duration of action.
  • Molecular weight: 376.45
  • Formula: C20H28N2O5
  • CLOGP: 1.96
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 0
  • TPSA: 76.15
  • ALOGS: -2.80
  • ROTB: 9

Drug dosage:

None

Approvals:

DateAgencyCompanyOrphan
July 12, 1996 FDA MYLAN INSTITUTIONAL

FDA Adverse Event Reporting System

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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
Low birth weight baby 422.70 104.31 73 1082 1597 3383107
Foetal exposure during pregnancy 404.07 104.31 103 1052 15448 3369256
Anaphylactic shock 349.61 104.31 76 1079 5663 3379041
Unwanted awareness during anaesthesia 237.16 104.31 32 1123 110 3384594
Delayed recovery from anaesthesia 219.32 104.31 33 1122 282 3384422
Cardiac arrest 199.96 104.31 68 1087 27251 3357453
Bradycardia 198.00 104.31 60 1095 16609 3368095
Hypotension 167.33 104.31 70 1085 49444 3335260
Respiratory depression 157.90 104.31 37 1118 3797 3380907
Generalised erythema 127.60 104.31 28 1127 2133 3382571
Post procedural complication 123.33 104.31 32 1123 4985 3379719
Blood pressure decreased 123.02 104.31 40 1115 13796 3370908
Circulatory collapse 122.08 104.31 33 1122 6016 3378688

Pharmacologic Action:

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SourceCodeDescription
ATC N01AH06 NERVOUS SYSTEM
ANESTHETICS
ANESTHETICS, GENERAL
Opioid anesthetics
FDA MoA N0000175684 Full Opioid Agonists
FDA EPC N0000175690 Opioid Agonist
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 D006993 Hypnotics and Sedatives
MeSH PA D009294 Narcotics
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents
CHEBI has role CHEBI:55322 mu-opioid receptor agonist
CHEBI has role CHEBI:35482 opioid analgesic
CHEBI has role CHEBI:38877 intravenous anaesthetic
CHEBI has role CHEBI:35717 sedative

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
General anesthesia indication 50697003
Local anesthesia indication 386761002
Acute postoperative pain indication 107401000119105
Low blood pressure contraindication 45007003
Bradycardia contraindication 48867003
Decreased respiratory function contraindication 80954004

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.07 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Mu-type opioid receptor GPCR AGONIST WOMBAT-PK CHEMBL

External reference:

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IDSource
4024040 VUID
N0000022045 NUI
C0246631 UMLSCUI
7292 IUPHAR_LIGAND_ID
D01177 KEGG_DRUG
5V444H5WIC UNII
132539-07-2 SECONDARY_CAS_RN
DB00899 DRUGBANK_ID
CHEMBL1005 ChEMBL_ID
4024040 VANDF
N0000007442 NDFRT
N0000022045 NDFRT
006250 NDDF
d04034 MMSL
73032 RXNORM
108379008 SNOMEDCT_US
386839004 SNOMEDCT_US
181723 MMSL
60815 PUBCHEM_CID
CHEMBL1201120 ChEMBL_ID
6924 INN_ID
C071741 MESH_SUPPLEMENTAL_RECORD_UI
CHEBI:8802 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Remifentanil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 63323-723 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 18 sections
Remifentanil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 63323-724 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 18 sections
Remifentanil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 63323-725 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS ANDA 18 sections
Ultiva HUMAN PRESCRIPTION DRUG LABEL 1 67457-198 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS NDA 18 sections