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

Stem definition	Drug id	CAS RN
opioid receptor agonists, analgesics, fentanyl derivatives	2363	132875-61-7

Description:

Molecule	Description
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 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

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

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)	37 mL/min/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	0.80 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.40 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.30 %	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	0.10 %	Benet LZ, Broccatelli F, Oprea TI

Showing 1 to 6 of 6 entries

Previous1Next

Approvals:

Date	Agency	Company	Orphan
July 12, 1996	FDA	MYLAN INSTITUTIONAL
Oct. 20, 2006	PMDA	Janssen Pharmaceutical K.K.

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
Anaphylactic shock	805.66	33.23	206	4003	23427	63461386
Anaphylactic reaction	341.11	33.23	137	4072	65963	63418850
Cardiac arrest	150.63	33.23	87	4122	92458	63392355
Delayed recovery from anaesthesia	136.16	33.23	26	4183	745	63484068
Bronchospasm	132.70	33.23	48	4161	17232	63467581
Bradycardia	127.56	33.23	72	4137	73155	63411658
Hypotension	126.50	33.23	120	4089	272484	63212329
Circulatory collapse	111.12	33.23	45	4164	21893	63462920
Neuromuscular block prolonged	81.65	33.23	16	4193	526	63484287
Serotonin syndrome	74.88	33.23	37	4172	28645	63456168

Showing 1 to 10 of 31 entries

Previous1 2 3 4Next

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
Anaphylactic shock	595.90	30.48	171	4192	15770	34936798
Anaphylactic reaction	232.69	30.48	102	4261	32199	34920369
Hyperthermia malignant	200.90	30.48	48	4315	2129	34950439
Cardiac arrest	151.31	30.48	112	4251	96047	34856521
Diabetes insipidus	143.68	30.48	39	4324	2889	34949679
Hypotension	143.42	30.48	156	4207	221493	34731075
Bradycardia	130.24	30.48	93	4270	75325	34877243
Delayed recovery from anaesthesia	129.97	30.48	28	4335	773	34951795
Trigemino-cardiac reflex	107.80	30.48	19	4344	174	34952394
Neuromuscular block prolonged	101.26	30.48	21	4342	480	34952088

Showing 1 to 10 of 37 entries

Previous1 2 3 4Next

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
Anaphylactic shock	1353.28	26.47	375	8173	35621	79700219
Anaphylactic reaction	557.46	26.47	239	8309	83504	79652336
Cardiac arrest	282.74	26.47	194	8354	171902	79563938
Delayed recovery from anaesthesia	248.85	26.47	53	8495	1620	79734220
Hypotension	247.51	26.47	268	8280	440049	79295791
Hyperthermia malignant	240.22	26.47	57	8491	2860	79732980
Bradycardia	227.60	26.47	155	8393	135402	79600438
Bronchospasm	198.59	26.47	81	8467	24778	79711062
Diabetes insipidus	179.68	26.47	51	8497	5186	79730654
Neuromuscular block prolonged	166.74	26.47	35	8513	995	79734845

Showing 1 to 10 of 72 entries

Previous1 2 3 4 5…8Next

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Show entries

Search:

Source	Code	Description
ATC	N01AH06	NERVOUS SYSTEM ANESTHETICS ANESTHETICS, GENERAL Opioid anesthetics
CHEBI has role	CHEBI:35482	narcotic analgesic
CHEBI has role	CHEBI:35717	hypnotics
CHEBI has role	CHEBI:38877	intravenous anesthetics
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
MeSH PA	D002491	Central Nervous System Agents

Showing 1 to 10 of 14 entries

Previous1 2Next

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

Show entries

Search:

Disease	Relation	SNOMED_ID
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

Showing 1 to 6 of 6 entries

Previous1Next

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.07	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])	Mechanism action	Bioact source	MoA source
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN	AGONIST				WOMBAT-PK	CHEMBL
Mu-type opioid receptor	GPCR		OPRM_RAT		IC50	9.22		CHEMBL

Showing 1 to 2 of 2 entries

Previous1Next

External reference:

Show entries

Search:

ID	Source
006250	NDDF
006251	NDDF
108376001	SNOMEDCT_US
108379008	SNOMEDCT_US
132539-07-2	SECONDARY_CAS_RN
181723	MMSL
186043	MMSL
236540	RXNORM
386839004	SNOMEDCT_US
4020990	VANDF

Showing 1 to 10 of 26 entries

Previous1 2 3Next

Pharmaceutical products:

Show entries

Search:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
REMIFENTANIL HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9391	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	1 mg	INTRAVENOUS	ANDA	28 sections
REMIFENTANIL HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9391	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	1 mg	INTRAVENOUS	ANDA	28 sections
REMIFENTANIL HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9392	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	2 mg	INTRAVENOUS	ANDA	28 sections
REMIFENTANIL HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9392	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	2 mg	INTRAVENOUS	ANDA	28 sections
REMIFENTANIL HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9393	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	5 mg	INTRAVENOUS	ANDA	28 sections
REMIFENTANIL HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9393	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	5 mg	INTRAVENOUS	ANDA	28 sections
Remifentanil Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	63323-723	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	1 mg	INTRAVENOUS	ANDA	30 sections
Remifentanil Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	63323-723	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	1 mg	INTRAVENOUS	ANDA	30 sections
Remifentanil Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	63323-724	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	1 mg	INTRAVENOUS	ANDA	30 sections
Remifentanil Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	63323-725	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	1 mg	INTRAVENOUS	ANDA	30 sections

Showing 1 to 10 of 24 entries

Previous1 2 3Next