Stem definition | Drug id | CAS RN |
---|---|---|
opioid receptor agonists, analgesics, fentanyl derivatives | 2491 | 56030-54-7 |
None
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 |
Date | Agency | Company | Orphan |
---|---|---|---|
May 4, 1984 | FDA | AKORN |
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 | 1257.88 | 29.72 | 317 | 4955 | 19957 | 46660833 |
Hypotension | 264.58 | 29.72 | 214 | 5058 | 232375 | 46448415 |
Bronchospasm | 242.47 | 29.72 | 84 | 5188 | 15623 | 46665167 |
Exposure during pregnancy | 144.85 | 29.72 | 110 | 5162 | 108102 | 46572688 |
Maternal exposure during delivery | 115.23 | 29.72 | 25 | 5247 | 791 | 46679999 |
Anaphylactoid shock | 113.75 | 29.72 | 21 | 5251 | 284 | 46680506 |
Anaphylactic reaction | 113.36 | 29.72 | 72 | 5200 | 53040 | 46627750 |
Tachycardia | 100.71 | 29.72 | 86 | 5186 | 99536 | 46581254 |
Circulatory collapse | 94.63 | 29.72 | 47 | 5225 | 21577 | 46659213 |
Cardiac arrest | 75.32 | 29.72 | 70 | 5202 | 90329 | 46590461 |
Shock | 74.04 | 29.72 | 40 | 5232 | 21805 | 46658985 |
Oliguria | 70.03 | 29.72 | 29 | 5243 | 8730 | 46672060 |
Hepatocellular injury | 67.89 | 29.72 | 42 | 5230 | 29480 | 46651310 |
Hepatorenal failure | 65.45 | 29.72 | 15 | 5257 | 611 | 46680179 |
Respiratory depression | 65.33 | 29.72 | 30 | 5242 | 11570 | 46669220 |
Peripheral nerve injury | 61.44 | 29.72 | 13 | 5259 | 364 | 46680426 |
Delayed recovery from anaesthesia | 60.70 | 29.72 | 15 | 5257 | 846 | 46679944 |
Haemodynamic instability | 59.81 | 29.72 | 25 | 5247 | 7700 | 46673090 |
Suspected product quality issue | 58.32 | 29.72 | 11 | 5261 | 168 | 46680622 |
Spinal epidural haemorrhage | 56.93 | 29.72 | 10 | 5262 | 100 | 46680690 |
Hypocapnia | 55.88 | 29.72 | 12 | 5260 | 361 | 46680429 |
Type I hypersensitivity | 54.04 | 29.72 | 17 | 5255 | 2329 | 46678461 |
Erythema | 50.65 | 29.72 | 71 | 5201 | 142749 | 46538041 |
Ventricular fibrillation | 47.36 | 29.72 | 24 | 5248 | 11472 | 46669318 |
Unwanted awareness during anaesthesia | 47.05 | 29.72 | 10 | 5262 | 286 | 46680504 |
Bradycardia | 46.98 | 29.72 | 47 | 5225 | 66251 | 46614539 |
Stress cardiomyopathy | 46.56 | 29.72 | 21 | 5251 | 7763 | 46673027 |
Patent ductus arteriosus | 45.73 | 29.72 | 17 | 5255 | 3845 | 46676945 |
Fatigue | 43.88 | 29.72 | 8 | 5264 | 608689 | 46072101 |
Foetal exposure during pregnancy | 42.62 | 29.72 | 32 | 5240 | 30715 | 46650075 |
Serotonin syndrome | 42.27 | 29.72 | 29 | 5243 | 24191 | 46656599 |
Oxygen saturation decreased | 40 | 29.72 | 44 | 5228 | 69120 | 46611670 |
Cauda equina syndrome | 39.03 | 29.72 | 10 | 5262 | 653 | 46680137 |
Anaesthetic complication | 37.04 | 29.72 | 12 | 5260 | 1805 | 46678985 |
Acute generalised exanthematous pustulosis | 36.89 | 29.72 | 19 | 5253 | 9386 | 46671404 |
Epidural haemorrhage | 36.35 | 29.72 | 7 | 5265 | 120 | 46680670 |
Cardio-respiratory arrest | 36.21 | 29.72 | 39 | 5233 | 59830 | 46620960 |
Myoglobin blood increased | 35.56 | 29.72 | 11 | 5261 | 1425 | 46679365 |
Paralysis | 35.31 | 29.72 | 18 | 5254 | 8703 | 46672087 |
Cholestasis | 35.09 | 29.72 | 27 | 5245 | 26866 | 46653924 |
Post procedural stroke | 34.25 | 29.72 | 6 | 5266 | 59 | 46680731 |
Foetal growth restriction | 33.91 | 29.72 | 16 | 5256 | 6551 | 46674239 |
Eosinophilia | 33.51 | 29.72 | 23 | 5249 | 19194 | 46661596 |
Suspected product contamination | 32.21 | 29.72 | 5 | 5267 | 21 | 46680769 |
Metabolic acidosis | 32.17 | 29.72 | 30 | 5242 | 38750 | 46642040 |
Carcinoid crisis | 31.63 | 29.72 | 7 | 5265 | 243 | 46680547 |
Diarrhoea | 31.51 | 29.72 | 12 | 5260 | 559590 | 46121200 |
Haemodilution | 31.26 | 29.72 | 6 | 5266 | 101 | 46680689 |
Foetal heart rate abnormal | 30.89 | 29.72 | 8 | 5264 | 545 | 46680245 |
Maternal exposure during pregnancy | 30.54 | 29.72 | 47 | 5225 | 102502 | 46578288 |
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 | 811.05 | 31.83 | 216 | 3907 | 13777 | 29934578 |
Bronchospasm | 170.10 | 31.83 | 61 | 4062 | 10277 | 29938078 |
Hypertransaminasaemia | 133.32 | 31.83 | 40 | 4083 | 3845 | 29944510 |
Anaphylactic reaction | 111.75 | 31.83 | 61 | 4062 | 27921 | 29920434 |
Hypotension | 105.08 | 31.83 | 133 | 3990 | 200432 | 29747923 |
Hyperthermia malignant | 104.19 | 31.83 | 28 | 4095 | 1806 | 29946549 |
Tachycardia | 75.76 | 31.83 | 70 | 4053 | 73669 | 29874686 |
Circulatory collapse | 69.57 | 31.83 | 40 | 4083 | 20174 | 29928181 |
Toxic epidermal necrolysis | 68.50 | 31.83 | 38 | 4085 | 17902 | 29930453 |
Septic shock | 58.82 | 31.83 | 57 | 4066 | 63550 | 29884805 |
Haemodynamic instability | 57.33 | 31.83 | 26 | 4097 | 7989 | 29940366 |
Rhabdomyolysis | 56.97 | 31.83 | 56 | 4067 | 63524 | 29884831 |
Multiple organ dysfunction syndrome | 53.33 | 31.83 | 54 | 4069 | 63433 | 29884922 |
Shock | 52.59 | 31.83 | 35 | 4088 | 22824 | 29925531 |
Victim of crime | 50.75 | 31.83 | 11 | 4112 | 282 | 29948073 |
Hepatorenal failure | 47.77 | 31.83 | 12 | 4111 | 592 | 29947763 |
Anaphylactoid shock | 46.86 | 31.83 | 11 | 4112 | 407 | 29947948 |
Hepatocellular injury | 44.60 | 31.83 | 33 | 4090 | 25438 | 29922917 |
Type I hypersensitivity | 42.40 | 31.83 | 12 | 4111 | 936 | 29947419 |
Patent ductus arteriosus | 42.10 | 31.83 | 16 | 4107 | 3153 | 29945202 |
Erythema | 41.27 | 31.83 | 52 | 4071 | 77399 | 29870956 |
Suspected product contamination | 39.13 | 31.83 | 7 | 4116 | 63 | 29948292 |
Coma | 38.76 | 31.83 | 37 | 4086 | 40412 | 29907943 |
Infantile apnoea | 38.62 | 31.83 | 11 | 4112 | 878 | 29947477 |
Suspected product quality issue | 38.52 | 31.83 | 8 | 4115 | 166 | 29948189 |
Stress cardiomyopathy | 36.59 | 31.83 | 12 | 4111 | 1537 | 29946818 |
Fear | 36.10 | 31.83 | 21 | 4102 | 10804 | 29937551 |
Injury | 35.47 | 31.83 | 27 | 4096 | 21704 | 29926651 |
Post procedural haemorrhage | 33.62 | 31.83 | 18 | 4105 | 7892 | 29940463 |
Fibrinolysis increased | 33.06 | 31.83 | 5 | 4118 | 13 | 29948342 |
Agitation neonatal | 32.76 | 31.83 | 10 | 4113 | 1015 | 29947340 |
Anaesthetic complication | 32.35 | 31.83 | 10 | 4113 | 1059 | 29947296 |
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 | narcotic analgesics |
CHEBI has role | CHEBI:38877 | intravenous anesthetics |
CHEBI has role | CHEBI:55322 | mu opioid agonist |
CHEBI has role | CHEBI:60807 | anaesthesia adjuvants |
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 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 8.37 | Basic |
None
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 |
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 |
ID | Source |
---|---|
4019936 | VUID |
N0000148021 | NUI |
D00845 | KEGG_DRUG |
60561-17-3 | SECONDARY_CAS_RN |
4019269 | VANDF |
4019936 | VANDF |
C0143993 | UMLSCUI |
CHEBI:9316 | CHEBI |
CHEMBL658 | ChEMBL_ID |
CHEMBL1201163 | ChEMBL_ID |
D017409 | MESH_DESCRIPTOR_UI |
3534 | IUPHAR_LIGAND_ID |
4048 | INN_ID |
DB00708 | DRUGBANK_ID |
AFE2YW0IIZ | UNII |
41693 | PUBCHEM_CID |
56795 | RXNORM |
10199 | MMSL |
32203 | MMSL |
5519 | MMSL |
d00378 | MMSL |
001570 | NDDF |
004630 | NDDF |
370275005 | SNOMEDCT_US |
37527009 | SNOMEDCT_US |
49998007 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Sufentanil Citrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-3382 | INJECTION, SOLUTION | 50 ug | EPIDURAL | ANDA | 32 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 |
Dsuvia | Human Prescription Drug Label | 1 | 61621-430 | TABLET | 30 ug | SUBLINGUAL | NDA | 30 sections |