alfentanil indications/contra

Stem definitionDrug idCAS RN
opioid receptor agonists, analgesics, fentanyl derivatives 114 71195-58-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • alfentanil
  • alfentanil hydrochloride
  • afentanyl
  • alfentanyl
  • rapifen
  • alfentanil HCl
A short-acting opioid anesthetic and analgesic derivative of FENTANYL. It produces an early peak analgesic effect and fast recovery of consciousness. Alfentanil is effective as an anesthetic during surgery, for supplementation of analgesia during surgical procedures, and as an analgesic for critically ill patients.
  • Molecular weight: 416.53
  • Formula: C21H32N6O3
  • CLOGP: 2.13
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 0
  • TPSA: 81.05
  • ALOGS: -3.22
  • ROTB: 9

Drug dosage:

None

Approvals:

DateAgencyCompanyOrphan
Dec. 29, 1986 FDA AKORN

FDA Adverse Event Reporting System

None

Pharmacologic Action:

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SourceCodeDescription
ATC N01AH02 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 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:38877 intravenous anaesthetic
CHEBI has role CHEBI:35488 central nervous system depressant
CHEBI has role CHEBI:49110 peripheral nervous system drug

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
General anesthesia indication 50697003
Asthenia contraindication 13791008
Chronic disease of respiratory system contraindication 17097001
Low blood pressure contraindication 45007003
Bradycardia contraindication 48867003
Benign intracranial hypertension contraindication 68267002 DOID:11459
Injury of head contraindication 82271004
Kidney disease contraindication 90708001 DOID:2527
Disease of liver contraindication 235856003 DOID:409
Lesion of brain contraindication 301766008
Pain off-label use 22253000
Sedation in Intubated Patients off-label use

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.71 Basic
pKa2 0.12 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 EC50 8.50 WOMBAT-PK CHEMBL
Multidrug resistance protein 1 Transporter IC50 3.95 WOMBAT-PK
Mu-type opioid receptor GPCR IC50 7.82 CHEMBL
Opioid receptor GPCR Ki 8.09 CHEMBL
Mu-type opioid receptor GPCR Ki 8.09 CHEMBL

External reference:

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IDSource
4019597 VUID
N0000147693 NUI
C0002026 UMLSCUI
7108 IUPHAR_LIGAND_ID
D00835 KEGG_DRUG
CHEMBL634 ChEMBL_ID
11S92G0TIW UNII
70879-28-6 SECONDARY_CAS_RN
4818 INN_ID
DB00802 DRUGBANK_ID
480 RXNORM
387560008 SNOMEDCT_US
96183007 SNOMEDCT_US
4147 MMSL
d00167 MMSL
4019597 VANDF
N0000147693 NDFRT
N0000006447 NDFRT
004631 NDDF
51263 PUBCHEM_CID
CHEMBL1200531 ChEMBL_ID
D015760 MESH_DESCRIPTOR_UI
CHEBI:2569 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Alfentanil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0409-2266 INJECTION, SOLUTION 500 ug INTRAVENOUS ANDA 18 sections
Alfentanil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 17478-067 INJECTION 500 ug INTRAVENOUS NDA 17 sections
Alfentanil HUMAN PRESCRIPTION DRUG LABEL 1 17478-841 INJECTION 500 ug INTRAVENOUS NDA 14 sections