Scroll

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

Stem definition	Drug id	CAS RN
opioid receptor agonists, analgesics, fentanyl derivatives	114	71195-58-9

Description:

Molecule	Description
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

Molecule

Description

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:

Show entries

Search:

Property	Value	Reference
CL (Clearance)	3.90 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.60 hours	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	1 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	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
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	0.45 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.09 %	Lombardo F, Berellini G, Obach RS

Showing 1 to 8 of 8 entries

Previous1Next

Approvals:

Date	Agency	Company	Orphan
Dec. 29, 1986	FDA	AKORN

FDA Adverse Event Reporting System (Female)

Show entries

Search:

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

Showing 1 to 1 of 1 entries

Previous1Next

FDA Adverse Event Reporting System (Male)

Show entries

Search:

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	113.57	47.47	34	708	21612	34934577

Showing 1 to 1 of 1 entries

Previous1Next

FDA Adverse Event Reporting System (Geriatric)

Show entries

Search:

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	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

Showing 1 to 5 of 5 entries

Previous1Next

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Show entries

Search:

Source	Code	Description
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 EPC	N0000175690	Opioid Agonist
FDA MoA	N0000175684	Full Opioid Agonists
MeSH PA	D000700	Analgesics
MeSH PA	D000701	Analgesics, Opioid

Showing 1 to 10 of 17 entries

Previous1 2Next

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

Show entries

Search:

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

Showing 1 to 10 of 12 entries

Previous1 2Next

🐶 Veterinary Drug Use

None

🐶 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:

Show entries

Search:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN	AGONIST	EC50	8.50	WOMBAT-PK	CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		IC50	3.95	WOMBAT-PK
Mu-type opioid receptor	GPCR		OPRM_RAT		Ki	8.09	CHEMBL
Mu-type opioid receptor	GPCR		OPRM_CAVPO		IC50	7.82	CHEMBL
Opioid receptor	GPCR		OPRD_RAT OPRM_RAT OPRK_RAT SGMR1_RAT		Ki	8.09	CHEMBL

Showing 1 to 5 of 5 entries

Previous1Next

External reference:

Show entries

Search:

ID	Source
001571	NDDF
004631	NDDF
1670	MMSL
1N74HM2BS7	UNII
203203	RXNORM
387560008	SNOMEDCT_US
4019322	VANDF
4019597	VUID
4019597	VANDF
41329	MMSL

Showing 1 to 10 of 26 entries

Previous1 2 3Next

Pharmaceutical products:

Show entries

Search:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Alfentanil	HUMAN PRESCRIPTION DRUG LABEL	1	17478-841	INJECTION	500 ug	INTRAVENOUS	NDA	22 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 Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	17478-067	INJECTION	500 ug	INTRAVENOUS	NDA	27 sections

Showing 1 to 4 of 4 entries

Previous1Next