meprobamate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| tranquillizers, propanediol and pentanediol derivatives | 1704 | 57-53-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A carbamate with hypnotic, sedative, and some muscle relaxant properties, although in therapeutic doses reduction of anxiety rather than a direct effect may be responsible for muscle relaxation. Meprobamate has been reported to have anticonvulsant actions against petit mal seizures, but not against grand mal seizures (which may be exacerbated). It is used in the treatment of ANXIETY DISORDERS, and also for the short-term management of INSOMNIA but has largely been superseded by the BENZODIAZEPINES. (From Martindale, The Extra Pharmacopoeia, 30th ed, p603)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1.20 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 3.40 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 157.09 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 0.70 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 0.60 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 1 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 14 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 28, 1955 | FDA | MEDPOINTE PHARM HLC |
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 |
|---|---|---|---|---|---|---|
| Toxicity to various agents | 425.47 | 43.75 | 172 | 1326 | 247078 | 63240446 |
| Accidental overdose | 181.43 | 43.75 | 51 | 1447 | 23258 | 63464266 |
| Drug abuse | 174.49 | 43.75 | 65 | 1433 | 72453 | 63415071 |
| Completed suicide | 130.81 | 43.75 | 65 | 1433 | 145608 | 63341916 |
| Overdose | 117.16 | 43.75 | 56 | 1442 | 115022 | 63372502 |
| Accidental death | 101.41 | 43.75 | 20 | 1478 | 1956 | 63485568 |
| Respiratory arrest | 73.63 | 43.75 | 28 | 1470 | 32617 | 63454907 |
| Unresponsive to stimuli | 62.11 | 43.75 | 25 | 1473 | 33791 | 63453733 |
| Pulmonary oedema | 56.53 | 43.75 | 27 | 1471 | 54846 | 63432678 |
| Cardiac arrest | 56.40 | 43.75 | 32 | 1466 | 92513 | 63395011 |
| Drug screen positive | 47.45 | 43.75 | 12 | 1486 | 3617 | 63483907 |
| Sciatica | 45.07 | 43.75 | 20 | 1478 | 34304 | 63453220 |
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 |
|---|---|---|---|---|---|---|
| Toxicity to various agents | 214.89 | 63.60 | 96 | 635 | 200266 | 34755934 |
| Drug abuse | 185.36 | 63.60 | 71 | 660 | 99025 | 34857175 |
| Accidental overdose | 167.02 | 63.60 | 45 | 686 | 20095 | 34936105 |
| Respiratory arrest | 113.68 | 63.60 | 36 | 695 | 28007 | 34928193 |
| Cardiac arrest | 73.62 | 63.60 | 37 | 694 | 96122 | 34860078 |
| Overdose | 63.71 | 63.60 | 33 | 698 | 91026 | 34865174 |
FDA Adverse Event Reporting System (Geriatric)
| 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 |
|---|---|---|---|---|---|---|
| Toxicity to various agents | 534.62 | 44.59 | 245 | 1882 | 421295 | 79320966 |
| Drug abuse | 337.51 | 44.59 | 135 | 1992 | 162556 | 79579705 |
| Accidental overdose | 317.54 | 44.59 | 91 | 2036 | 39490 | 79702771 |
| Overdose | 181.31 | 44.59 | 91 | 2036 | 184115 | 79558146 |
| Respiratory arrest | 162.30 | 44.59 | 60 | 2067 | 57490 | 79684771 |
| Completed suicide | 140.83 | 44.59 | 85 | 2042 | 245682 | 79496579 |
| Cardiac arrest | 115.43 | 44.59 | 66 | 2061 | 172030 | 79570231 |
| Accidental death | 93.92 | 44.59 | 22 | 2105 | 4269 | 79737992 |
| Pulmonary oedema | 76 | 44.59 | 40 | 2087 | 88214 | 79654047 |
| Pulmonary congestion | 64.45 | 44.59 | 25 | 2102 | 27075 | 79715186 |
| Cardio-respiratory arrest | 63.03 | 44.59 | 38 | 2089 | 108472 | 79633789 |
| Unresponsive to stimuli | 58.79 | 44.59 | 29 | 2098 | 55759 | 79686502 |
| Drug screen positive | 57.73 | 44.59 | 16 | 2111 | 6047 | 79736214 |
| Poisoning | 45.19 | 44.59 | 19 | 2108 | 25253 | 79717008 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N05BC01 | NERVOUS SYSTEM PSYCHOLEPTICS ANXIOLYTICS Carbamates |
| ATC | N05BC51 | NERVOUS SYSTEM PSYCHOLEPTICS ANXIOLYTICS Carbamates |
| ATC | N05CX01 | NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Hypnotics and sedatives in combination, excl. barbiturates |
| MeSH PA | D014151 | Anti-Anxiety Agents |
| MeSH PA | D000927 | Anticonvulsants |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D006993 | Hypnotics and Sedatives |
| 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 | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Anxiety | indication | 48694002 | |
| Anxiety associated with Menopause | indication | ||
| Pain with Tension and Anxiety | indication | ||
| Hyperlipoproteinemia | contraindication | 3744001 | DOID:1168 |
| Hypocalcemia | contraindication | 5291005 | |
| Suicidal thoughts | contraindication | 6471006 | |
| Alcoholism | contraindication | 7200002 | |
| Peptic ulcer | contraindication | 13200003 | DOID:750 |
| Hypercholesterolemia | contraindication | 13644009 | |
| Lowered convulsive threshold | contraindication | 19260006 | |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Chloasma | contraindication | 36209000 | |
| Migraine | contraindication | 37796009 | DOID:6364 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Disorder of gallbladder | contraindication | 39621005 | DOID:0060262 |
| Gastrointestinal ulcer | contraindication | 40845000 | |
| Hypothyroidism | contraindication | 40930008 | DOID:1459 |
| Body fluid retention | contraindication | 43498006 | |
| Thrombosis of retinal vein | contraindication | 46085004 | |
| Humoral hypercalcemia of malignancy | contraindication | 47709007 | |
| Dementia | contraindication | 52448006 | |
| Vitamin K deficiency | contraindication | 52675005 | DOID:11249 |
| Nasal polyp | contraindication | 52756005 | |
| Hepatic porphyria | contraindication | 55056006 | DOID:3133 |
| Systemic lupus erythematosus | contraindication | 55464009 | DOID:9074 |
| Acute nephropathy | contraindication | 58574008 | |
| Thrombophlebitis | contraindication | 64156001 | DOID:3875 |
| Intermenstrual bleeding - irregular | contraindication | 64996003 | |
| Substance abuse | contraindication | 66214007 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Factor II deficiency | contraindication | 73975000 | |
| Reye's syndrome | contraindication | 74351001 | DOID:14525 |
| Gastrointestinal hemorrhage | contraindication | 74474003 | |
| Thrombotic thrombocytopenic purpura | contraindication | 78129009 | DOID:10772 |
| Epilepsy | contraindication | 84757009 | DOID:1826 |
| Breast lump | contraindication | 89164003 | |
| Gout | contraindication | 90560007 | DOID:13189 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Hemophilia | contraindication | 90935002 | |
| Uterine leiomyoma | contraindication | 95315005 | DOID:13223 |
| Anemia due to enzyme deficiency | contraindication | 111577008 | |
| Deep venous thrombosis | contraindication | 128053003 | |
| von Willebrand disorder | contraindication | 128105004 | DOID:12531 |
| Seizure disorder | contraindication | 128613002 | |
| Endometriosis | contraindication | 129103003 | |
| Mammography abnormal | contraindication | 168750009 | |
| Asthma | contraindication | 195967001 | DOID:2841 |
| Cerebrovascular accident | contraindication | 230690007 | |
| Pulmonary thromboembolism | contraindication | 233935004 | |
| Acute intermittent porphyria | contraindication | 234422006 | DOID:3890 |
| Thrombophilia | contraindication | 234467004 | DOID:2452 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Endometrial carcinoma | contraindication | 254878006 | DOID:2871 |
| Chorea | contraindication | 271700006 | |
| Anemia | contraindication | 271737000 | DOID:2355 |
| Pregnancy, function | contraindication | 289908002 | |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Hypertriglyceridemia | contraindication | 302870006 | |
| Functional visual loss | contraindication | 313165001 | |
| Malignant tumor of ovary | contraindication | 363443007 | DOID:2394 |
| Thromboembolic disorder | contraindication | 371039008 | |
| Cardiovascular event risk | contraindication | 395112001 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Disorder of coronary artery | contraindication | 414024009 | |
| Obesity | contraindication | 414916001 | DOID:9970 |
| Estrogen receptor positive tumor | contraindication | 416053008 | |
| Family history of malignant neoplasm of breast | contraindication | 429740004 | |
| Hypertensive urgency | contraindication | 443482000 | |
| Acute erosive gastritis | contraindication | 444926003 | |
| Carcinoma of female breast | contraindication | 447782002 | |
| Smokes tobacco daily | contraindication | 449868002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
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 |
|---|---|---|---|---|---|---|---|---|---|
| GABA-A receptor alpha-2/beta-3/gamma-2 | Ion channel | AGONIST | WOMBAT-PK | CHEMBL | |||||
| GABA-A receptor alpha-3/beta-3/gamma-2 | Ion channel | AGONIST | WOMBAT-PK | CHEMBL | |||||
| GABA-A receptor alpha-5/beta-3/gamma-2 | Ion channel | AGONIST | WOMBAT-PK | CHEMBL | |||||
| GABA-A receptor alpha-1/beta-3/gamma-2 | Ion channel | AGONIST | WOMBAT-PK | CHEMBL | |||||
| Multidrug resistance protein 1 | Transporter | IC50 | 6.82 | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4017913 | VUID |
| N0000146264 | NUI |
| D00376 | KEGG_DRUG |
| 4017913 | VANDF |
| C0025386 | UMLSCUI |
| CHEBI:6761 | CHEBI |
| CHEMBL979 | ChEMBL_ID |
| DB00371 | DRUGBANK_ID |
| D008620 | MESH_DESCRIPTOR_UI |
| 4064 | PUBCHEM_CID |
| 7225 | IUPHAR_LIGAND_ID |
| 533 | INN_ID |
| 9I7LNY769Q | UNII |
| 6760 | RXNORM |
| 1904 | MMSL |
| 5051 | MMSL |
| d00288 | MMSL |
| 001445 | NDDF |
| 387395007 | SNOMEDCT_US |
| 70864001 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| MEPROBAMATE | Human Prescription Drug Label | 1 | 46708-019 | TABLET | 200 mg | ORAL | ANDA | 12 sections |
| MEPROBAMATE | Human Prescription Drug Label | 1 | 46708-019 | TABLET | 200 mg | ORAL | ANDA | 12 sections |
| MEPROBAMATE | Human Prescription Drug Label | 1 | 46708-020 | TABLET | 400 mg | ORAL | ANDA | 12 sections |
| MEPROBAMATE | Human Prescription Drug Label | 1 | 46708-020 | TABLET | 400 mg | ORAL | ANDA | 12 sections |
| Meprobamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51672-4147 | TABLET | 200 mg | ORAL | ANDA | 14 sections |
| Meprobamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51672-4148 | TABLET | 400 mg | ORAL | ANDA | 14 sections |
| Meprobamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52549-4147 | TABLET | 200 mg | ORAL | ANDA | 17 sections |
| Meprobamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52549-4148 | TABLET | 400 mg | ORAL | ANDA | 17 sections |
| Meprobamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55111-640 | TABLET | 200 mg | ORAL | ANDA | 12 sections |
| Meprobamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55111-641 | TABLET | 400 mg | ORAL | ANDA | 12 sections |
| Meprobamate | Human Prescription Drug Label | 1 | 62332-019 | TABLET | 200 mg | ORAL | ANDA | 12 sections |
| Meprobamate | Human Prescription Drug Label | 1 | 62332-020 | TABLET | 400 mg | ORAL | ANDA | 12 sections |
| Meprobamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69097-974 | TABLET | 200 mg | ORAL | ANDA | 13 sections |
| Meprobamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69097-975 | TABLET | 400 mg | ORAL | ANDA | 13 sections |