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

Stem definition	Drug id	CAS RN
opioid receptor agonists, analgesics, fentanyl derivatives	2491	56030-54-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: sulfentanyl sulfentanil sulfentanil citrate sufentanil sufentanil citrate	An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent. Molecular weight: 386.55 Formula: C22H30N2O2S CLOGP: 3.59 LIPINSKI: 0 HAC: 4 HDO: 0 TPSA: 32.78 ALOGS: -4.51 ROTB: 8 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

sulfentanyl
sulfentanil
sulfentanil citrate
sufentanil
sufentanil citrate

An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent.

Molecular weight: 386.55
Formula: C22H30N2O2S
CLOGP: 3.59
LIPINSKI: 0
HAC: 4
HDO: 0
TPSA: 32.78
ALOGS: -4.51
ROTB: 8

Status: OFP

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

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
Vd (Volume of distribution)	9.40 L/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	6 %	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	15 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	14 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.08 %	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.06 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	0 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

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Approvals:

Date	Agency	Company	Orphan
June 25, 2018	EMA	LABORATOIRE AGUETTANT
May 4, 1984	FDA	AKORN

FDA Adverse Event Reporting System (Female)

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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	1777.17	29.56	430	6640	23203	63458749
Hypotension	326.01	29.56	257	6813	272347	63209605
Bronchospasm	270.17	29.56	93	6977	17187	63464765
Anaphylactic reaction	231.68	29.56	123	6947	65977	63415975
Maternal exposure during delivery	179.42	29.56	40	7030	1460	63480492
Exposure during pregnancy	156.38	29.56	133	6937	155414	63326538
Cardiac arrest	142.72	29.56	102	6968	92443	63389509
Anaphylactoid shock	111.94	29.56	21	7049	316	63481636
Circulatory collapse	106.58	29.56	51	7019	21887	63460065
Tachycardia	106.44	29.56	95	6975	118061	63363891

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FDA Adverse Event Reporting System (Male)

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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	1151.54	30.58	300	5101	15641	34935889
Bronchospasm	190.35	30.58	69	5332	10662	34940868
Hyperthermia malignant	180.77	30.58	46	5355	2131	34949399
Hypotension	136.73	30.58	169	5232	221480	34730050
Anaphylactic reaction	133.69	30.58	75	5326	32226	34919304
Hypertransaminasaemia	114.31	30.58	40	5361	5566	34945964
Toxic epidermal necrolysis	111.11	30.58	58	5343	21588	34929942
Rash maculo-papular	109.45	30.58	63	5338	28388	34923142
Tachycardia	101.02	30.58	92	5309	84680	34866850
Eosinophilia	84.98	30.58	52	5349	26170	34925360

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FDA Adverse Event Reporting System (Geriatric)

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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	2865.51	27.40	723	10912	35273	79697480
Bronchospasm	446.77	27.40	159	11476	24700	79708053
Anaphylactic reaction	361.61	27.40	196	11439	83547	79649206
Hypotension	318.04	27.40	354	11281	439963	79292790
Tachycardia	199.59	27.40	182	11453	177586	79555167
Hyperthermia malignant	193.63	27.40	51	11584	2866	79729887
Circulatory collapse	175.89	27.40	93	11542	37575	79695178
Cardiac arrest	169.71	27.40	164	11471	171932	79560821
Maternal exposure during delivery	167.62	27.40	39	11596	1307	79731446
Type I hypersensitivity	155.54	27.40	47	11588	4351	79728402

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N01AH03	NERVOUS SYSTEM ANESTHETICS ANESTHETICS, GENERAL Opioid anesthetics
CHEBI has role	CHEBI:35482	narcotic analgesic
CHEBI has role	CHEBI:38877	intravenous anesthetics
CHEBI has role	CHEBI:55322	mu-opioid agonists
CHEBI has role	CHEBI:60807	anaesthestic adjuvant
FDA EPC	N0000175690	Opioid Agonist
FDA MoA	N0000175684	Full Opioid Agonists
MeSH PA	D000759	Adjuvants, Anesthesia
MeSH PA	D000700	Analgesics
MeSH PA	D000701	Analgesics, Opioid

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

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Disease	Relation	SNOMED_ID	DOID
General anesthesia	indication	50697003
Postoperative pain	indication	213299007
Asthenia	contraindication	13791008
Chronic disease of respiratory system	contraindication	17097001
Decreased cardiac function	contraindication	43650005
Bradycardia	contraindication	48867003
Injury of head	contraindication	82271004
Kidney disease	contraindication	90708001	DOID:557
Disease of liver	contraindication	235856003	DOID:409

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.37	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 0.03MG BASE	DSUVIA	VERTICAL PHARMS	N209128	Nov. 2, 2018	RX	TABLET	SUBLINGUAL	10245228	Jan. 5, 2027	TREATMENT OF ACUTE PAIN
EQ 0.03MG BASE	DSUVIA	VERTICAL PHARMS	N209128	Nov. 2, 2018	RX	TABLET	SUBLINGUAL	10507180	Jan. 5, 2027	TREATMENT OF ACUTE PAIN
EQ 0.03MG BASE	DSUVIA	VERTICAL PHARMS	N209128	Nov. 2, 2018	RX	TABLET	SUBLINGUAL	8226978	Jan. 5, 2027	TREATMENT OF ACUTE PAIN
EQ 0.03MG BASE	DSUVIA	VERTICAL PHARMS	N209128	Nov. 2, 2018	RX	TABLET	SUBLINGUAL	8535714	Jan. 5, 2027	TREATMENT OF ACUTE PAIN
EQ 0.03MG BASE	DSUVIA	VERTICAL PHARMS	N209128	Nov. 2, 2018	RX	TABLET	SUBLINGUAL	8778393	Jan. 5, 2027	TREATMENT OF ACUTE PAIN
EQ 0.03MG BASE	DSUVIA	VERTICAL PHARMS	N209128	Nov. 2, 2018	RX	TABLET	SUBLINGUAL	8778394	Jan. 5, 2027	TREATMENT OF ACUTE PAIN
EQ 0.03MG BASE	DSUVIA	VERTICAL PHARMS	N209128	Nov. 2, 2018	RX	TABLET	SUBLINGUAL	8865211	Jan. 5, 2027	TREATMENT OF ACUTE PAIN
EQ 0.03MG BASE	DSUVIA	VERTICAL PHARMS	N209128	Nov. 2, 2018	RX	TABLET	SUBLINGUAL	9320710	Jan. 5, 2027	TREATMENT OF ACUTE PAIN
EQ 0.03MG BASE	DSUVIA	VERTICAL PHARMS	N209128	Nov. 2, 2018	RX	TABLET	SUBLINGUAL	8202535	Oct. 22, 2030	TREATMENT OF ACUTE PAIN
EQ 0.03MG BASE	DSUVIA	VERTICAL PHARMS	N209128	Nov. 2, 2018	RX	TABLET	SUBLINGUAL	8865743	Oct. 22, 2030	TREATMENT OF ACUTE PAIN

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN	AGONIST	EC50	8.13	WOMBAT-PK	CHEMBL
Kappa-type opioid receptor	GPCR	P41145	OPRK_HUMAN		EC50	6.70	WOMBAT-PK
Delta-type opioid receptor	GPCR	P41143	OPRD_HUMAN		Ki	7.30	PDSP
Solute carrier family 22 member 1	Transporter	O15245	S22A1_HUMAN		IC50	4.71	CHEMBL
Mu-type opioid receptor	GPCR		OPRM_RAT		Ki	9.66	CHEMBL
Sigma non-opioid intracellular receptor 1	Membrane other		SGMR1_CAVPO		IC50	5.68	CHEMBL
Opioid receptor	GPCR		OPRD_RAT OPRM_RAT OPRK_RAT SGMR1_RAT		Ki	10.70	CHEMBL

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External reference:

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ID	Source
001570	NDDF
004630	NDDF
10199	MMSL
32203	MMSL
3534	IUPHAR_LIGAND_ID
370275005	SNOMEDCT_US
37527009	SNOMEDCT_US
4019269	VANDF
4019936	VUID
4019936	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Dsuvia	Human Prescription Drug Label	1	61621-430	TABLET	30 ug	SUBLINGUAL	NDA	30 sections
Sufentanil Citrate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-3382	INJECTION, SOLUTION	50 ug	EPIDURAL	ANDA	33 sections
Sufentanil Citrate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-3382	INJECTION, SOLUTION	50 ug	EPIDURAL	ANDA	33 sections
Sufentanil Citrate	HUMAN PRESCRIPTION DRUG LABEL	1	0641-6110	INJECTION	0.05 mg	EPIDURAL	ANDA	27 sections
Sufentanil Citrate	HUMAN PRESCRIPTION DRUG LABEL	1	0641-6111	INJECTION	0.05 mg	EPIDURAL	ANDA	27 sections
Sufentanil Citrate	HUMAN PRESCRIPTION DRUG LABEL	1	0641-6112	INJECTION	0.05 mg	EPIDURAL	ANDA	27 sections
Sufentanil Citrate	HUMAN PRESCRIPTION DRUG LABEL	1	17478-050	INJECTION	50 ug	INTRAVENOUS	NDA	29 sections
Sufentanil Citrate	HUMAN PRESCRIPTION DRUG LABEL	1	17478-050	INJECTION	50 ug	INTRAVENOUS	NDA	29 sections

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