cyclobenzaprine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 751 | 303-53-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
structurally related to tricyclic antidepressants relieves skeletal muscle spasm of local origin without interfering with muscle function, it is ineffective in muscle spasm due to central nervous system disease
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 |
| S (Water solubility) | 200 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0.50 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 1.37 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 55 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 26, 1977 | 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 |
|---|---|---|---|---|---|---|
| Completed suicide | 4490.12 | 70.96 | 904 | 1453 | 20130 | 2335598 |
| Toxicity to various agents | 2598.48 | 70.96 | 634 | 1723 | 32120 | 2323608 |
| Drug abuse | 1735.93 | 70.96 | 383 | 1974 | 11643 | 2344085 |
| Respiratory arrest | 890.26 | 70.96 | 198 | 2159 | 5980 | 2349748 |
| Cardio-respiratory arrest | 818.10 | 70.96 | 199 | 2158 | 8947 | 2346781 |
| Cardiac arrest | 815.56 | 70.96 | 219 | 2138 | 14711 | 2341017 |
| Death | 443.13 | 70.96 | 216 | 2141 | 81252 | 2274476 |
| Intentional product misuse | 431.23 | 70.96 | 121 | 2236 | 9368 | 2346360 |
| Poisoning | 407.64 | 70.96 | 91 | 2266 | 2729 | 2352999 |
| Drug hypersensitivity | 365.87 | 70.96 | 160 | 2197 | 46483 | 2309245 |
| Overdose | 323.86 | 70.96 | 116 | 2241 | 19791 | 2335937 |
| Intentional overdose | 229.94 | 70.96 | 78 | 2279 | 11243 | 2344485 |
| Temperature regulation disorder | 201.01 | 70.96 | 32 | 2325 | 129 | 2355599 |
| Somnolence | 171.44 | 70.96 | 77 | 2280 | 23408 | 2332320 |
| Decorticate posture | 165.64 | 70.96 | 23 | 2334 | 23 | 2355705 |
| Food allergy | 157.36 | 70.96 | 32 | 2325 | 599 | 2355129 |
| Coeliac disease | 154.20 | 70.96 | 33 | 2324 | 799 | 2354929 |
| Hypotension | 142.04 | 70.96 | 75 | 2282 | 32361 | 2323367 |
| Immunodeficiency | 140.34 | 70.96 | 32 | 2325 | 1044 | 2354684 |
| Unresponsive to stimuli | 136.88 | 70.96 | 43 | 2314 | 4833 | 2350895 |
| Bursitis | 136.71 | 70.96 | 35 | 2322 | 1873 | 2353855 |
| Suicide attempt | 132.61 | 70.96 | 52 | 2305 | 11230 | 2344498 |
| Constipation | 120.79 | 70.96 | 59 | 2298 | 21570 | 2334158 |
| Coma | 107.28 | 70.96 | 42 | 2315 | 9014 | 2346714 |
| Myocardial depression | 102.46 | 70.96 | 16 | 2341 | 55 | 2355673 |
| Asthma | 98.23 | 70.96 | 42 | 2315 | 11272 | 2344456 |
| Urinary incontinence | 92.94 | 70.96 | 31 | 2326 | 4202 | 2351526 |
| Respiratory depression | 90.53 | 70.96 | 26 | 2331 | 2144 | 2353584 |
| Serotonin syndrome | 90.13 | 70.96 | 29 | 2328 | 3511 | 2352217 |
| Exposure via ingestion | 89.76 | 70.96 | 21 | 2336 | 767 | 2354961 |
| Electrocardiogram QRS complex prolonged | 87.72 | 70.96 | 22 | 2335 | 1080 | 2354648 |
| Rash erythematous | 86.14 | 70.96 | 32 | 2325 | 5944 | 2349784 |
| Drug interaction | 85.64 | 70.96 | 52 | 2305 | 29111 | 2326617 |
| Sedation | 83.37 | 70.96 | 27 | 2330 | 3335 | 2352393 |
| Fluid retention | 81.02 | 70.96 | 32 | 2325 | 7014 | 2348714 |
| Encephalopathy | 79.09 | 70.96 | 28 | 2329 | 4533 | 2351195 |
| Depressed level of consciousness | 78.66 | 70.96 | 32 | 2325 | 7572 | 2348156 |
| Seizure | 75.35 | 70.96 | 45 | 2312 | 24421 | 2331307 |
| Hepatic enzyme increased | 74.02 | 70.96 | 33 | 2324 | 9769 | 2345959 |
| Upper respiratory tract infection | 73.97 | 70.96 | 32 | 2325 | 8819 | 2346909 |
| Loss of consciousness | 72.43 | 70.96 | 40 | 2317 | 18727 | 2337001 |
| Drug screen positive | 71.40 | 70.96 | 18 | 2339 | 902 | 2354826 |
| Hyperhidrosis | 71.09 | 70.96 | 37 | 2320 | 15385 | 2340343 |
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 |
|---|---|---|---|---|---|---|
| Completed suicide | 1709.67 | 96.32 | 388 | 920 | 15924 | 1729549 |
| Toxicity to various agents | 1235.28 | 96.32 | 337 | 971 | 28804 | 1716669 |
| Drug abuse | 1014.98 | 96.32 | 249 | 1059 | 13440 | 1732033 |
| Respiratory arrest | 435.69 | 96.32 | 108 | 1200 | 5731 | 1739742 |
| Cardio-respiratory arrest | 358.45 | 96.32 | 102 | 1206 | 9191 | 1736282 |
| Cardiac arrest | 340.71 | 96.32 | 111 | 1197 | 15819 | 1729654 |
| Intentional product misuse | 257.29 | 96.32 | 75 | 1233 | 7283 | 1738190 |
| Overdose | 245.22 | 96.32 | 88 | 1220 | 16613 | 1728860 |
| Death | 230.44 | 96.32 | 139 | 1169 | 87304 | 1658169 |
| Poisoning | 120.70 | 96.32 | 33 | 1275 | 2499 | 1742974 |
| Intentional overdose | 114.10 | 96.32 | 41 | 1267 | 7629 | 1737844 |
| Depressed level of consciousness | 108.51 | 96.32 | 38 | 1270 | 6554 | 1738919 |
| Coma | 101.18 | 96.32 | 37 | 1271 | 7225 | 1738248 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | M03BX08 | MUSCULO-SKELETAL SYSTEM MUSCLE RELAXANTS MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS Other centrally acting agents |
| FDA PE | N0000175730 | Centrally-mediated Muscle Relaxation |
| CHEBI has role | CHEBI:51371 | muscle relaxant |
| CHEBI has role | CHEBI:35473 | tranquilizing drug |
| CHEBI has role | CHEBI:35469 | antidepressant |
| MeSH PA | D000928 | Antidepressive Agents |
| MeSH PA | D000929 | Antidepressive Agents, Tricyclic |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D009125 | Muscle Relaxants, Central |
| MeSH PA | D009465 | Neuromuscular Agents |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D011619 | Psychotropic Drugs |
| MeSH PA | D014149 | Tranquilizing Agents |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Spasticity | indication | 221360009 | |
| Fibromyalgia | off-label use | 203082005 | DOID:631 |
| Sinus tachycardia | contraindication | 11092001 | |
| Glaucoma | contraindication | 23986001 | DOID:1686 |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Chronic heart failure | contraindication | 48447003 | |
| Hepatic failure | contraindication | 59927004 | |
| Open-angle glaucoma | contraindication | 84494001 | DOID:1067 |
| Heart block | contraindication | 233916004 | |
| Retention of urine | contraindication | 267064002 | |
| Myocardial infarction in recovery phase | contraindication | 418044006 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.66 | 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 15MG | AMRIX | TEVA PHARMS INTL | N021777 | Feb. 1, 2007 | RX | CAPSULE, EXTENDED RELEASE | ORAL | 7544372 | Nov. 14, 2023 | RELIEF OF MUSCLE SPASM |
| 15MG | AMRIX | TEVA PHARMS INTL | N021777 | Feb. 1, 2007 | RX | CAPSULE, EXTENDED RELEASE | ORAL | 7829121 | Nov. 14, 2023 | RELIEF OF MUSCLE SPASM |
| 15MG | AMRIX | TEVA PHARMS INTL | N021777 | Feb. 1, 2007 | RX | CAPSULE, EXTENDED RELEASE | ORAL | 8877245 | Nov. 14, 2023 | RELIEF OF MUSCLE SPASM |
| 15MG | AMRIX | TEVA PHARMS INTL | N021777 | Feb. 1, 2007 | RX | CAPSULE, EXTENDED RELEASE | ORAL | 9375410 | Nov. 14, 2023 | RELIEF OF MUSCLE SPASM |
| 15MG | AMRIX | TEVA PHARMS INTL | N021777 | Feb. 1, 2007 | RX | CAPSULE, EXTENDED RELEASE | ORAL | 9399025 | Nov. 14, 2023 | RELIEF OF MUSCLE SPASM |
| 30MG | AMRIX | TEVA PHARMS INTL | N021777 | Feb. 1, 2007 | RX | CAPSULE, EXTENDED RELEASE | ORAL | 7544372 | Nov. 14, 2023 | RELIEF OF MUSCLE SPASM |
| 30MG | AMRIX | TEVA PHARMS INTL | N021777 | Feb. 1, 2007 | RX | CAPSULE, EXTENDED RELEASE | ORAL | 7829121 | Nov. 14, 2023 | RELIEF OF MUSCLE SPASM |
| 30MG | AMRIX | TEVA PHARMS INTL | N021777 | Feb. 1, 2007 | RX | CAPSULE, EXTENDED RELEASE | ORAL | 8877245 | Nov. 14, 2023 | RELIEF OF MUSCLE SPASM |
| 30MG | AMRIX | TEVA PHARMS INTL | N021777 | Feb. 1, 2007 | RX | CAPSULE, EXTENDED RELEASE | ORAL | 9375410 | Nov. 14, 2023 | RELIEF OF MUSCLE SPASM |
| 30MG | AMRIX | TEVA PHARMS INTL | N021777 | Feb. 1, 2007 | RX | CAPSULE, EXTENDED RELEASE | ORAL | 9399025 | Nov. 14, 2023 | RELIEF OF MUSCLE SPASM |
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 |
|---|---|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 2A | GPCR | ANTAGONIST | Ki | 7.54 | WOMBAT-PK | CHEMBL | |||
| 5-hydroxytryptamine receptor 2C | GPCR | ANTAGONIST | Ki | 7.24 | WOMBAT-PK | ||||
| Aldehyde oxidase | Enzyme | IC50 | 5.51 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | IC50 | 6.95 | WOMBAT-PK | |||||
| Histamine H1 receptor | GPCR | Ki | 8.83 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 7 | GPCR | Ki | 6.82 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 6 | GPCR | Ki | 6.84 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 2B | GPCR | Ki | 6.81 | WOMBAT-PK | |||||
| Sodium-dependent noradrenaline transporter | Transporter | Ki | 7.44 | WOMBAT-PK | |||||
| Sodium-dependent serotonin transporter | Transporter | Ki | 6.97 | WOMBAT-PK | |||||
| Multidrug resistance protein 1 | Transporter | IC50 | 4.73 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M2 | GPCR | Ki | 7.22 | PDSP | |||||
| Muscarinic acetylcholine receptor M3 | GPCR | Ki | 8.22 | PDSP | |||||
| Proto-oncogene tyrosine-protein kinase receptor Ret | Kinase | IC50 | 6.52 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019699 | VUID |
| N0000147791 | NUI |
| C0056732 | UMLSCUI |
| D00772 | KEGG_DRUG |
| 0VE05JYS2P | UNII |
| 6202-23-9 | SECONDARY_CAS_RN |
| 791 | INN_ID |
| 80802008 | SNOMEDCT_US |
| 4019699 | VANDF |
| d00963 | MMSL |
| 21949 | RXNORM |
| 373779004 | SNOMEDCT_US |
| 004680 | NDDF |
| CHEBI:3996 | CHEBI |
| CHEMBL669 | ChEMBL_ID |
| DB00924 | DRUGBANK_ID |
| CHEMBL1200636 | ChEMBL_ID |
| 7152 | IUPHAR_LIGAND_ID |
| 2895 | PUBCHEM_CID |
| C004704 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-1920 | CAPSULE, EXTENDED RELEASE | 15 mg | ORAL | NDA AUTHORIZED GENERIC | 19 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-1921 | CAPSULE, EXTENDED RELEASE | 30 mg | ORAL | NDA AUTHORIZED GENERIC | 19 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0115-1436 | CAPSULE, EXTENDED RELEASE | 15 mg | ORAL | NDA AUTHORIZED GENERIC | 19 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0115-1437 | CAPSULE, EXTENDED RELEASE | 30 mg | ORAL | NDA AUTHORIZED GENERIC | 19 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-0751 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 12 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-0761 | TABLET, FILM COATED | 7.50 mg | ORAL | ANDA | 12 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-0771 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 12 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0440-1350 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 12 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0440-7350 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 11 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-3256 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 12 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-3330 | TABLET, FILM COATED | 7.50 mg | ORAL | ANDA | 12 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-5658 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 12 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0615-3520 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 14 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0615-7528 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 14 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0615-8084 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 13 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0615-8182 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 13 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0904-7809 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 12 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10544-072 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 12 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10544-159 | TABLET | 10 mg | ORAL | ANDA | 14 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10544-200 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 13 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10702-006 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 13 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10702-007 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 13 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 12634-528 | TABLET | 10 mg | ORAL | ANDA | 12 sections |
| CYCLOBENZAPRINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-065 | TABLET | 10 mg | ORAL | ANDA | 13 sections |
| CYCLOBENZAPRINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-544 | TABLET | 5 mg | ORAL | ANDA | 12 sections |
| Amrix | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-596 | CAPSULE, EXTENDED RELEASE | 15 mg | ORAL | NDA | 13 sections |
| FEXMID | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-699 | TABLET, FILM COATED | 7.50 mg | ORAL | ANDA | 13 sections |
| Amrix | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-810 | CAPSULE, EXTENDED RELEASE | 30 mg | ORAL | NDA | 13 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-036 | TABLET | 5 mg | ORAL | ANDA | 14 sections |
| Cyclobenzaprine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-037 | TABLET | 10 mg | ORAL | ANDA | 14 sections |