sufentanil 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 |
|---|---|
|
Synonyms:
|
An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent.
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) | 6 % | Benet LZ, Broccatelli F, Oprea TI |
| 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 |
| Vd (Volume of distribution) | 9.40 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 15 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.08 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 14 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 4, 1984 | 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 | 856.67 | 91.84 | 147 | 564 | 4139 | 2353235 |
| Hypotension | 407.26 | 91.84 | 115 | 596 | 32321 | 2325053 |
| Exposure during pregnancy | 276.85 | 91.84 | 81 | 630 | 25138 | 2332236 |
| Bronchospasm | 180.18 | 91.84 | 38 | 673 | 2986 | 2354388 |
| Anaphylactoid shock | 114.46 | 91.84 | 16 | 695 | 96 | 2357278 |
| Drug ineffective | 108.43 | 91.84 | 61 | 650 | 101563 | 2255811 |
| Circulatory collapse | 92.57 | 91.84 | 23 | 688 | 3697 | 2353677 |
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 |
|---|---|---|---|---|---|---|
| Anaphylactic shock | 451.94 | 82.58 | 81 | 362 | 2818 | 1743520 |
| Bronchospasm | 128.18 | 82.58 | 27 | 416 | 2055 | 1744283 |
| Hypotension | 119.05 | 82.58 | 45 | 398 | 29609 | 1716729 |
| Anaphylactic reaction | 99.26 | 82.58 | 27 | 416 | 6086 | 1740252 |
| Circulatory collapse | 83.63 | 82.58 | 21 | 422 | 3446 | 1742892 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N01AH03 | NERVOUS SYSTEM ANESTHETICS ANESTHETICS, GENERAL Opioid anesthetics |
| MeSH PA | D000759 | Adjuvants, Anesthesia |
| 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 |
| CHEBI has role | CHEBI:35482 | opioid analgesic |
| CHEBI has role | CHEBI:55322 | mu-opioid receptor agonist |
| CHEBI has role | CHEBI:60807 | anaesthesia adjuvant |
| CHEBI has role | CHEBI:38877 | intravenous anaesthetic |
Drug Use (View source of the data)
| 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 |
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)
| 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 | ACELRX PHARMS | N209128 | Nov. 2, 2018 | RX | TABLET | SUBLINGUAL | 10245228 | Jan. 5, 2027 | TREATMENT OF ACUTE PAIN |
| EQ 0.03MG BASE | DSUVIA | ACELRX PHARMS | N209128 | Nov. 2, 2018 | RX | TABLET | SUBLINGUAL | 10507180 | Jan. 5, 2027 | TREATMENT OF ACUTE PAIN |
| EQ 0.03MG BASE | DSUVIA | ACELRX PHARMS | N209128 | Nov. 2, 2018 | RX | TABLET | SUBLINGUAL | 8226978 | Jan. 5, 2027 | TREATMENT OF ACUTE PAIN |
| EQ 0.03MG BASE | DSUVIA | ACELRX PHARMS | N209128 | Nov. 2, 2018 | RX | TABLET | SUBLINGUAL | 8535714 | Jan. 5, 2027 | TREATMENT OF ACUTE PAIN |
| EQ 0.03MG BASE | DSUVIA | ACELRX PHARMS | N209128 | Nov. 2, 2018 | RX | TABLET | SUBLINGUAL | 8778393 | Jan. 5, 2027 | TREATMENT OF ACUTE PAIN |
| EQ 0.03MG BASE | DSUVIA | ACELRX PHARMS | N209128 | Nov. 2, 2018 | RX | TABLET | SUBLINGUAL | 8778394 | Jan. 5, 2027 | TREATMENT OF ACUTE PAIN |
| EQ 0.03MG BASE | DSUVIA | ACELRX PHARMS | N209128 | Nov. 2, 2018 | RX | TABLET | SUBLINGUAL | 8865211 | Jan. 5, 2027 | TREATMENT OF ACUTE PAIN |
| EQ 0.03MG BASE | DSUVIA | ACELRX PHARMS | N209128 | Nov. 2, 2018 | RX | TABLET | SUBLINGUAL | 9320710 | Jan. 5, 2027 | TREATMENT OF ACUTE PAIN |
| EQ 0.03MG BASE | DSUVIA | ACELRX PHARMS | N209128 | Nov. 2, 2018 | RX | TABLET | SUBLINGUAL | 8202535 | Oct. 22, 2030 | TREATMENT OF ACUTE PAIN |
| EQ 0.03MG BASE | DSUVIA | ACELRX PHARMS | N209128 | Nov. 2, 2018 | RX | TABLET | SUBLINGUAL | 8865743 | Oct. 22, 2030 | TREATMENT OF ACUTE PAIN |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 0.03MG BASE | DSUVIA | ACELRX PHARMS | N209128 | Nov. 2, 2018 | RX | TABLET | SUBLINGUAL | Nov. 2, 2021 | NEW PRODUCT |
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 | 8.13 | WOMBAT-PK | CHEMBL | |||
| Delta-type opioid receptor | GPCR | Ki | 7.30 | PDSP | |||||
| Kappa-type opioid receptor | GPCR | EC50 | 6.70 | WOMBAT-PK | |||||
| Opioid receptor | GPCR | Ki | 10.70 | CHEMBL | |||||
| Mu-type opioid receptor | GPCR | Ki | 9.66 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019936 | VUID |
| N0000148021 | NUI |
| C0143993 | UMLSCUI |
| D00845 | KEGG_DRUG |
| 370275005 | SNOMEDCT_US |
| 4019936 | VANDF |
| 56795 | RXNORM |
| d00378 | MMSL |
| 004630 | NDDF |
| 49998007 | SNOMEDCT_US |
| AFE2YW0IIZ | UNII |
| 4048 | INN_ID |
| CHEMBL658 | ChEMBL_ID |
| DB00708 | DRUGBANK_ID |
| 60561-17-3 | SECONDARY_CAS_RN |
| CHEBI:9316 | CHEBI |
| CHEMBL1201163 | ChEMBL_ID |
| D017409 | MESH_DESCRIPTOR_UI |
| 41693 | PUBCHEM_CID |
| 3534 | IUPHAR_LIGAND_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Sufentanil Citrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-3382 | INJECTION, SOLUTION | 50 ug | EPIDURAL | ANDA | 19 sections |
| Sufentanil Citrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-6110 | INJECTION | 0.05 mg | EPIDURAL | ANDA | 17 sections |
| Sufentanil Citrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-6111 | INJECTION | 0.05 mg | EPIDURAL | ANDA | 17 sections |
| Sufentanil Citrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-6112 | INJECTION | 0.05 mg | EPIDURAL | ANDA | 17 sections |
| Sufentanil Citrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-050 | INJECTION | 50 ug | INTRAVENOUS | NDA | 18 sections |
| Dsuvia | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61621-430 | TABLET | 30 ug | SUBLINGUAL | NDA | 19 sections |