atracurium Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| neuromuscular blocking agents with rigid structure | 259 | 64228-79-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 0 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 8.50 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.65 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 0.10 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 5.70 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.52 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 0.31 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 23, 1983 | FDA |
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 | 275.73 | 138.47 | 52 | 355 | 4234 | 2353444 |
| Hypotension | 184.21 | 138.47 | 55 | 352 | 32381 | 2325297 |
| Anaphylactic reaction | 173.69 | 138.47 | 41 | 366 | 9664 | 2348014 |
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 |
|---|---|---|---|---|---|---|
| Bronchospasm | 179.37 | 109.58 | 33 | 247 | 2049 | 1744452 |
| Anaphylactic reaction | 154.83 | 109.58 | 35 | 245 | 6078 | 1740423 |
| Anaphylactic shock | 144.08 | 109.58 | 29 | 251 | 2870 | 1743631 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | M03AC04 | MUSCULO-SKELETAL SYSTEM MUSCLE RELAXANTS MUSCLE RELAXANTS, PERIPHERALLY ACTING AGENTS Other quaternary ammonium compounds |
| FDA PE | N0000175732 | Neuromuscular Nondepolarizing Blockade |
| FDA EPC | N0000175720 | Nondepolarizing Neuromuscular Blocker |
| MeSH PA | D018678 | Cholinergic Agents |
| MeSH PA | D018680 | Cholinergic Antagonists |
| MeSH PA | D009465 | Neuromuscular Agents |
| MeSH PA | D009466 | Neuromuscular Blocking Agents |
| MeSH PA | D003473 | Neuromuscular Nondepolarizing Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018733 | Nicotinic Antagonists |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| CHEBI has role | CHEBI:51371 | muscle relaxant |
| CHEBI has role | CHEBI:48878 | nicotinic antagonist |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Muscle relaxation, function | indication | 11977004 | |
| General anesthesia | indication | 50697003 | |
| Skeletal Muscle Relaxation for Endotracheal Intubation | indication | ||
| Hypocalcemia | contraindication | 5291005 | |
| Disorder of lung | contraindication | 19829001 | DOID:850 |
| Hypokalemia | contraindication | 43339004 | |
| Low blood pressure | contraindication | 45007003 | |
| Eaton-Lambert syndrome | contraindication | 56989000 | DOID:0050214 |
| Hypermagnesemia | contraindication | 66978005 | |
| Myasthenia gravis | contraindication | 91637004 | DOID:437 |
| Disorder of electrolytes | contraindication | 237840007 | |
| Hypothermia | contraindication | 386689009 | |
| Malignant hyperthermia | contraindication | 405501007 |
Acid dissociation constants calculated using MoKa v3.0.0
None
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Acetylcholine receptor | Ion channel | ANTAGONIST | IC50 | 7.77 | WOMBAT-PK | CHEMBL | |||
| Neuronal acetylcholine receptor subunit alpha-2 | Ion channel | WOMBAT-PK | |||||||
| Small conductance calcium-activated potassium channel protein 3 | Ion channel | Ki | 5.23 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D001279 | MESH_DESCRIPTOR_UI |
| 4019619 | VUID |
| N0000147713 | NUI |
| C0004234 | UMLSCUI |
| D00758 | KEGG_DRUG |
| 40AX66P76P | UNII |
| 4734 | INN_ID |
| 64228-81-5 | SECONDARY_CAS_RN |
| 74074008 | SNOMEDCT_US |
| 4019619 | VANDF |
| 1218 | RXNORM |
| 372835000 | SNOMEDCT_US |
| d00173 | MMSL |
| 013420 | NDDF |
| CHEMBL1360 | ChEMBL_ID |
| DB00732 | DRUGBANK_ID |
| CHEMBL1200527 | ChEMBL_ID |
| CHEBI:2914 | CHEBI |
| 9537 | IUPHAR_LIGAND_ID |
| 47319 | PUBCHEM_CID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Atracurium Besylate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-1105 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 12 sections |
| Atracurium Besylate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-1109 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 12 sections |
| Atracurium Besylate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 25021-659 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 12 sections |
| Atracurium Besylate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 25021-672 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 12 sections |
| Atracurium Besylate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55150-216 | INJECTION, SOLUTION | 50 mg | INTRAVENOUS | ANDA | 12 sections |
| Atracurium Besylate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55150-217 | INJECTION, SOLUTION | 100 mg | INTRAVENOUS | ANDA | 12 sections |
| Atracurium Besylate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71288-701 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 12 sections |
| Atracurium Besylate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71288-702 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 12 sections |