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alfentanil ๐ถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| opioid receptor agonists, analgesics, fentanyl derivatives | 114 | 71195-58-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 ยตM/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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK7,NTRK2,PDK2,PDK4,PIK3CB,PRKDC,TEK | 19 | |||
| kinase-selectivity-class | GRK2 | 1 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 29, 1986 | FDA | AKORN |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Anaphylactic shock | 76.06 | 52.89 | 23 | 889 | 31594 | 90595941 |
| Epilepsy with myoclonic-atonic seizures | 62.91 | 52.89 | 8 | 904 | 105 | 90627430 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Toxic epidermal necrolysis | 102.83 | 48.74 | 33 | 855 | 26717 | 42593730 |
| Anaphylactic shock | 74.14 | 48.74 | 25 | 863 | 23492 | 42596955 |
| Methaemoglobinaemia | 72.45 | 48.74 | 18 | 870 | 5756 | 42614691 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Anaphylactic shock | 146.01 | 37.96 | 48 | 1817 | 51498 | 110535936 |
| Toxic epidermal necrolysis | 85.08 | 37.96 | 33 | 1832 | 56694 | 110530740 |
| Methaemoglobinaemia | 63.13 | 37.96 | 17 | 1848 | 9151 | 110578283 |
| Anaphylactic reaction | 62.92 | 37.96 | 33 | 1832 | 114267 | 110473167 |
| Epilepsy with myoclonic-atonic seizures | 58.55 | 37.96 | 8 | 1857 | 108 | 110587326 |
| Cardiac arrest | 55.85 | 37.96 | 37 | 1828 | 196716 | 110390718 |
| Change in seizure presentation | 42.78 | 37.96 | 8 | 1857 | 826 | 110586608 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N01AH02 | NERVOUS SYSTEM ANESTHETICS ANESTHETICS, GENERAL Opioid anesthetics |
| CHEBI has role | CHEBI:35482 | opioid analgesic |
| CHEBI has role | CHEBI:35488 | central nervous system depressant |
| CHEBI has role | CHEBI:38877 | intravenous anaesthetic |
| CHEBI has role | CHEBI:49110 | peripheral nervous system drug |
| CHEBI has role | CHEBI:55322 | ฮผ-opioid receptor agonist |
| MeSH PA | D000700 | Analgesics |
| MeSH PA | D000701 | Analgesics, Opioid |
| MeSH PA | D000777 | Anesthetics |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D009294 | Narcotics |
| MeSH PA | D018686 | Anesthetics, Intravenous |
| MeSH PA | D018689 | Sensory System Agents |
| FDA MoA | N0000175684 | Full Opioid Agonists |
| FDA EPC | N0000175690 | Opioid Agonist |
| CHEBI has role | CHEBI:38867 | anaesthetic |
Related Drugs by ATC class:
N01AH Opioid anesthetics 5 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 |
๐ถ Veterinary Drug Use
None
๐ถ Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 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 |
| 41329 | MMSL |
| 4147 | MMSL |
| d00167 | MMSL |
| 4019322 | VANDF |
| 4019597 | VANDF |
| 001571 | NDDF |
| 004631 | NDDF |
| 387560008 | SNOMEDCT_US |
| 96183007 | SNOMEDCT_US |
| 96184001 | SNOMEDCT_US |
| 1N74HM2BS7 | INXIGHT DRUGS |
Pharmaceutical products:
None