alfentanil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

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

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0.50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.59 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 1 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.45 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 3.90 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.09 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.60 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Dec. 29, 1986 FDA AKORN

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
Epilepsy with myoclonic-atonic seizures 62.27 58.10 8 685 105 63488224

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
Toxic epidermal necrolysis 113.57 47.47 34 708 21612 34934577

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
Toxic epidermal necrolysis 96.90 40.32 35 1462 44546 79698345
Anaphylactic shock 80.96 40.32 29 1468 35967 79706924
Epilepsy with myoclonic-atonic seizures 57.70 40.32 8 1489 108 79742783
Anaphylactic reaction 48.72 40.32 26 1471 83717 79659174
Change in seizure presentation 45.67 40.32 8 1489 514 79742377

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N01AH02 NERVOUS SYSTEM
ANESTHETICS
ANESTHETICS, GENERAL
Opioid anesthetics
CHEBI has role CHEBI:35482 narcotic analgesic
CHEBI has role CHEBI:35488 central nervous system depressants
CHEBI has role CHEBI:38877 intravenous anesthetics
CHEBI has role CHEBI:49110 peripheral nervous system drugs
CHEBI has role CHEBI:55322 mu-opioid agonists
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 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

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

DiseaseRelationSNOMED_IDDOID
General anesthesia indication 50697003
Pain off-label use 22253000
Sedation in Intubated Patients off-label use
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:557
Disease of liver contraindication 235856003 DOID:409
Lesion of brain contraindication 301766008




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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:

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 Ki 8.09 CHEMBL
Mu-type opioid receptor GPCR IC50 7.82 CHEMBL
Opioid receptor GPCR Ki 8.09 CHEMBL

External reference:

IDSource
4019597 VUID
N0000147693 NUI
D00835 KEGG_DRUG
70879-28-6 SECONDARY_CAS_RN
203203 RXNORM
C0002026 UMLSCUI
CHEBI:2569 CHEBI
CHEMBL634 ChEMBL_ID
CHEMBL1200531 ChEMBL_ID
D015760 MESH_DESCRIPTOR_UI
DB00802 DRUGBANK_ID
51263 PUBCHEM_CID
7108 IUPHAR_LIGAND_ID
4818 INN_ID
1N74HM2BS7 UNII
387560008 SNOMEDCT_US
96183007 SNOMEDCT_US
96184001 SNOMEDCT_US
4019322 VANDF
4019597 VANDF
1670 MMSL
41329 MMSL
4147 MMSL
d00167 MMSL
001571 NDDF
004631 NDDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Alfentanil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 17478-067 INJECTION 500 ug INTRAVENOUS NDA 27 sections
Alfentanil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 17478-067 INJECTION 500 ug INTRAVENOUS NDA 27 sections
Alfentanil Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 17478-067 INJECTION 500 ug INTRAVENOUS NDA 27 sections
Alfentanil HUMAN PRESCRIPTION DRUG LABEL 1 17478-841 INJECTION 500 ug INTRAVENOUS NDA 22 sections