rocuronium Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| neuromuscular blocking agents with rigid structure | 2396 | 119302-91-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Rocuronium bromide is a nondepolarizing neuromuscular blocking agent with a rapid to intermediate onset depending on dose and intermediate duration. It acts by competing for cholinergic receptors at the motor end-plate. This action is antagonized by acetylcholinesterase inhibitors, such as neostigmine and edrophonium.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 17 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.38 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 0.21 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 3.70 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.54 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.60 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 17, 1994 | FDA | ORGANON USA INC |
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 reaction | 1429.76 | 167.44 | 284 | 1062 | 9421 | 2347318 |
| Anaphylactic shock | 711.82 | 167.44 | 140 | 1206 | 4146 | 2352593 |
| Hypotension | 514.24 | 167.44 | 160 | 1186 | 32276 | 2324463 |
| Neuromuscular block prolonged | 480.33 | 167.44 | 61 | 1285 | 50 | 2356689 |
| Cardiac arrest | 479.77 | 167.44 | 128 | 1218 | 14802 | 2341937 |
| Bronchospasm | 477.65 | 167.44 | 95 | 1251 | 2929 | 2353810 |
| Tachycardia | 335.53 | 167.44 | 99 | 1247 | 16310 | 2340429 |
| Circulatory collapse | 304.48 | 167.44 | 68 | 1278 | 3652 | 2353087 |
| Delayed recovery from anaesthesia | 190.56 | 167.44 | 29 | 1317 | 163 | 2356576 |
| Oxygen saturation decreased | 177.38 | 167.44 | 51 | 1295 | 7535 | 2349204 |
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 reaction | 722.56 | 132.83 | 157 | 906 | 5956 | 1739762 |
| Anaphylactic shock | 576.64 | 132.83 | 115 | 948 | 2784 | 1742934 |
| Hypotension | 334.33 | 132.83 | 121 | 942 | 29533 | 1716185 |
| Neuromuscular block prolonged | 234.72 | 132.83 | 31 | 1032 | 27 | 1745691 |
| Bronchospasm | 213.14 | 132.83 | 48 | 1015 | 2034 | 1743684 |
| Cardiac arrest | 208.31 | 132.83 | 73 | 990 | 15857 | 1729861 |
| Hyperthermia malignant | 167.31 | 132.83 | 29 | 1034 | 300 | 1745418 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | M03AC09 | 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 | D009465 | Neuromuscular Agents |
| MeSH PA | D009466 | Neuromuscular Blocking Agents |
| MeSH PA | D003473 | Neuromuscular Nondepolarizing Agents |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| CHEBI has role | CHEBI:51372 | neuromuscular agent |
| CHEBI has role | CHEBI:51371 | muscle relaxant |
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 | ||
| Respiratory acidosis | contraindication | 12326000 | |
| Alkalosis | contraindication | 21420006 | |
| Acidosis | contraindication | 51387008 | |
| Eaton-Lambert syndrome | contraindication | 56989000 | DOID:0050214 |
| Pulmonary hypertension | contraindication | 70995007 | DOID:6432 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Myasthenia gravis | contraindication | 91637004 | DOID:437 |
| Respiratory alkalosis | contraindication | 111378004 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Disorder of electrolytes | contraindication | 237840007 | |
| Malignant hyperthermia | contraindication | 405501007 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.61 | Basic |
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 | |||
| Acetylcholine receptor; alpha1/beta1/delta/gamma | Ion channel | IC50 | 7.09 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D000077123 | MESH_DESCRIPTOR_UI |
| C0209337 | UMLSCUI |
| D00765 | KEGG_DRUG |
| 108449002 | SNOMEDCT_US |
| 013418 | NDDF |
| 372494005 | SNOMEDCT_US |
| 68139 | RXNORM |
| d03766 | MMSL |
| DB00728 | DRUGBANK_ID |
| CHEMBL1200648 | ChEMBL_ID |
| I65MW4OFHZ | UNII |
| 6864 | INN_ID |
| CHEBI:8885 | CHEBI |
| CHEMBL1201244 | ChEMBL_ID |
| 441290 | PUBCHEM_CID |
| 4003 | IUPHAR_LIGAND_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Rocuronium Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9250 | INJECTION | 10 mg | INTRAVENOUS | ANDA | 17 sections |
| Rocuronium Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9251 | INJECTION | 10 mg | INTRAVENOUS | ANDA | 17 sections |
| ROCURONIUM BROMIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-9558 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 17 sections |
| Rocuronium Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-3220 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 17 sections |
| rocuronium bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 25021-662 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 17 sections |
| rocuronium bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 39822-4200 | SOLUTION | 10 mg | INTRAVENOUS | ANDA | 18 sections |
| Rocuronium Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43066-007 | INJECTION | 50 mg | INTRAVENOUS | ANDA | 17 sections |
| Rocuronium Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43066-013 | INJECTION | 100 mg | INTRAVENOUS | ANDA | 17 sections |
| Rocuronium Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 47781-616 | INJECTION | 10 mg | INTRAVENOUS | ANDA | 16 sections |
| Rocuronium Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 47781-617 | INJECTION | 10 mg | INTRAVENOUS | ANDA | 16 sections |
| ROCURONIUM BROMIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1354 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 17 sections |
| ROCURONIUM BROMIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1355 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 17 sections |
| Rocuronium Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55150-225 | INJECTION, SOLUTION | 50 mg | INTRAVENOUS | ANDA | 17 sections |
| Rocuronium Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55150-226 | INJECTION, SOLUTION | 100 mg | INTRAVENOUS | ANDA | 17 sections |
| Rocuronium | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63323-426 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 17 sections |
| Rocuronium Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67457-228 | INJECTION | 10 mg | INTRAVENOUS | ANDA | 17 sections |
| Rocuronium Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68083-364 | INJECTION | 10 mg | INTRAVENOUS | ANDA | 17 sections |
| Rocuronium Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68083-365 | INJECTION | 10 mg | INTRAVENOUS | ANDA | 17 sections |
| Rocuronium Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70860-651 | SOLUTION | 10 mg | INTRAVENOUS | ANDA | 17 sections |
| Rocuronium bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71479-004 | INJECTION, SOLUTION | 100 mg | INTRAVENOUS | ANDA | 18 sections |
| Rocuronium bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71479-005 | INJECTION, SOLUTION | 50 mg | INTRAVENOUS | ANDA | 18 sections |
| rocuronium bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71872-7036 | SOLUTION | 10 mg | INTRAVENOUS | ANDA | 17 sections |
| rocuronium bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71872-7202 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 17 sections |
| Rocuronium Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71872-7207 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 17 sections |
| Rocuronium Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72611-756 | INJECTION | 10 mg | INTRAVENOUS | ANDA | 17 sections |
| Rocuronium Bromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72611-757 | INJECTION | 10 mg | INTRAVENOUS | ANDA | 17 sections |