primidone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2267 | 125-33-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A barbiturate derivative that acts as a GABA modulator and anti-epileptic agent. It is partly metabolized to PHENOBARBITAL in the body and owes some of its actions to this metabolite.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1.25 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.60 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 35 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 98.18 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 92 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 8, 1954 | FDA | VALEANT |
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 |
|---|---|---|---|---|---|---|
| Seizure | 145.46 | 14.44 | 127 | 7222 | 117747 | 50480028 |
| Fall | 64.89 | 14.44 | 147 | 7202 | 334785 | 50262990 |
| Ataxia | 50.57 | 14.44 | 29 | 7320 | 13757 | 50584018 |
| Tremor | 48.70 | 14.44 | 71 | 7278 | 114832 | 50482943 |
| Petit mal epilepsy | 44.22 | 14.44 | 17 | 7332 | 3272 | 50594503 |
| Completed suicide | 38.76 | 14.44 | 69 | 7280 | 131820 | 50465955 |
| Anticonvulsant drug level increased | 37.28 | 14.44 | 12 | 7337 | 1372 | 50596403 |
| Lennox-Gastaut syndrome | 34.39 | 14.44 | 8 | 7341 | 269 | 50597506 |
| Product complaint | 33.92 | 14.44 | 21 | 7328 | 11445 | 50586330 |
| Myoclonic epilepsy | 32.72 | 14.44 | 10 | 7339 | 965 | 50596810 |
| Drug interaction | 29.36 | 14.44 | 79 | 7270 | 199542 | 50398233 |
| Cerebellar atrophy | 27.41 | 14.44 | 8 | 7341 | 659 | 50597116 |
| Generalised tonic-clonic seizure | 23.95 | 14.44 | 24 | 7325 | 26286 | 50571489 |
| Diplopia | 22.16 | 14.44 | 20 | 7329 | 19240 | 50578535 |
| Somnolence | 21.43 | 14.44 | 60 | 7289 | 154925 | 50442850 |
| Anticonvulsant drug level above therapeutic | 20.41 | 14.44 | 6 | 7343 | 507 | 50597268 |
| Epilepsy | 20.23 | 14.44 | 20 | 7329 | 21547 | 50576228 |
| Gait disturbance | 18.74 | 14.44 | 56 | 7293 | 149949 | 50447826 |
| Nystagmus | 18.54 | 14.44 | 11 | 7338 | 5550 | 50592225 |
| Balance disorder | 18.27 | 14.44 | 35 | 7314 | 70555 | 50527220 |
| Dysarthria | 17.11 | 14.44 | 24 | 7325 | 37379 | 50560396 |
| Product substitution issue | 16.97 | 14.44 | 15 | 7334 | 14042 | 50583733 |
| Loss of consciousness | 16.02 | 14.44 | 42 | 7307 | 104311 | 50493464 |
| Multiple sclerosis | 15.61 | 14.44 | 17 | 7332 | 20476 | 50577299 |
| Urinary tract infection | 15.50 | 14.44 | 69 | 7280 | 223951 | 50373824 |
| Drug withdrawal convulsions | 14.71 | 14.44 | 6 | 7343 | 1347 | 50596428 |
| Dizziness | 14.58 | 14.44 | 93 | 7256 | 346276 | 50251499 |
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 |
|---|---|---|---|---|---|---|
| Serotonin syndrome | 56.96 | 17.02 | 36 | 4970 | 17476 | 29552045 |
| Ataxia | 55.35 | 17.02 | 31 | 4975 | 12072 | 29557449 |
| Seizure | 50.42 | 17.02 | 70 | 4936 | 93053 | 29476468 |
| Drug interaction | 40.21 | 17.02 | 97 | 4909 | 197288 | 29372233 |
| Gingival atrophy | 39.63 | 17.02 | 7 | 4999 | 46 | 29569475 |
| Somnolence | 38.47 | 17.02 | 62 | 4944 | 93893 | 29475628 |
| Fall | 32.80 | 17.02 | 84 | 4922 | 177094 | 29392427 |
| Open angle glaucoma | 32.70 | 17.02 | 7 | 4999 | 136 | 29569385 |
| Tremor | 32.11 | 17.02 | 50 | 4956 | 73488 | 29496033 |
| Bone metabolism disorder | 28.89 | 17.02 | 7 | 4999 | 240 | 29569281 |
| Plantar fascial fibromatosis | 28.50 | 17.02 | 4 | 5002 | 3 | 29569518 |
| Cervicobrachial syndrome | 27.90 | 17.02 | 7 | 4999 | 278 | 29569243 |
| Multiple-drug resistance | 26.42 | 17.02 | 13 | 4993 | 3887 | 29565634 |
| Developmental delay | 25.20 | 17.02 | 11 | 4995 | 2507 | 29567014 |
| Nystagmus | 22.35 | 17.02 | 12 | 4994 | 4297 | 29565224 |
| Drug ineffective | 20.09 | 17.02 | 117 | 4889 | 363053 | 29206468 |
| Acute kidney injury | 20.01 | 17.02 | 10 | 4996 | 265257 | 29304264 |
| Cerebellar atrophy | 19.80 | 17.02 | 6 | 5000 | 482 | 29569039 |
| Gastric hypomotility | 19.60 | 17.02 | 4 | 5002 | 61 | 29569460 |
| Balance disorder | 19.23 | 17.02 | 27 | 4979 | 36143 | 29533378 |
| Overdose | 19.23 | 17.02 | 42 | 4964 | 79777 | 29489744 |
| Generalised tonic-clonic seizure | 17.88 | 17.02 | 19 | 4987 | 19120 | 29550401 |
| Lens dislocation | 17.76 | 17.02 | 4 | 5002 | 99 | 29569422 |
| Jaw disorder | 17.61 | 17.02 | 8 | 4998 | 2002 | 29567519 |
| Gingival disorder | 17.41 | 17.02 | 7 | 4999 | 1299 | 29568222 |
| Visual field defect | 17.35 | 17.02 | 10 | 4996 | 4106 | 29565415 |
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 |
|---|---|---|---|---|---|---|
| Seizure | 102.38 | 14.44 | 124 | 9319 | 166768 | 64322521 |
| Ataxia | 95.80 | 14.44 | 52 | 9391 | 22032 | 64467257 |
| Fall | 77.58 | 14.44 | 181 | 9262 | 416645 | 64072644 |
| Completed suicide | 61.03 | 14.44 | 114 | 9329 | 224300 | 64264989 |
| Drug interaction | 56.41 | 14.44 | 147 | 9296 | 361936 | 64127353 |
| Tremor | 54.34 | 14.44 | 86 | 9357 | 148144 | 64341145 |
| Lennox-Gastaut syndrome | 41.65 | 14.44 | 9 | 9434 | 213 | 64489076 |
| Nystagmus | 38.33 | 14.44 | 21 | 9422 | 9047 | 64480242 |
| Gingival atrophy | 37.77 | 14.44 | 7 | 9436 | 73 | 64489216 |
| Cerebellar atrophy | 35.95 | 14.44 | 11 | 9432 | 1057 | 64488232 |
| Serotonin syndrome | 35.83 | 14.44 | 36 | 9407 | 39246 | 64450043 |
| Anticonvulsant drug level above therapeutic | 32.10 | 14.44 | 10 | 9433 | 1020 | 64488269 |
| Myoclonic epilepsy | 31.53 | 14.44 | 11 | 9432 | 1597 | 64487692 |
| Petit mal epilepsy | 30.95 | 14.44 | 15 | 9428 | 5017 | 64484272 |
| Epilepsy | 27.45 | 14.44 | 29 | 9414 | 33502 | 64455787 |
| Anticonvulsant drug level increased | 27.34 | 14.44 | 11 | 9432 | 2366 | 64486923 |
| Open angle glaucoma | 26.92 | 14.44 | 7 | 9436 | 372 | 64488917 |
| Generalised tonic-clonic seizure | 26.64 | 14.44 | 31 | 9412 | 39826 | 64449463 |
| Bone metabolism disorder | 26.03 | 14.44 | 7 | 9436 | 424 | 64488865 |
| Somnolence | 25.99 | 14.44 | 77 | 9366 | 203568 | 64285721 |
| Mental status changes | 24.49 | 14.44 | 37 | 9406 | 61125 | 64428164 |
| Plantar fascial fibromatosis | 23.83 | 14.44 | 4 | 9439 | 22 | 64489267 |
| Anticonvulsant drug level decreased | 22.90 | 14.44 | 9 | 9434 | 1821 | 64487468 |
| Choreoathetosis | 21.27 | 14.44 | 8 | 9435 | 1439 | 64487850 |
| Toxicity to various agents | 21.10 | 14.44 | 107 | 9336 | 363406 | 64125883 |
| Dysarthria | 21.09 | 14.44 | 34 | 9409 | 59372 | 64429917 |
| Dementia | 20.73 | 14.44 | 20 | 9423 | 20746 | 64468543 |
| Cervicobrachial syndrome | 20.09 | 14.44 | 7 | 9436 | 1012 | 64488277 |
| Inhibitory drug interaction | 19.89 | 14.44 | 10 | 9433 | 3617 | 64485672 |
| Balance disorder | 19.54 | 14.44 | 40 | 9403 | 83886 | 64405403 |
| Confusional state | 18.90 | 14.44 | 82 | 9361 | 261062 | 64228227 |
| Gingival disorder | 17.70 | 14.44 | 9 | 9434 | 3335 | 64485954 |
| Oesophageal ulcer | 17.34 | 14.44 | 11 | 9432 | 6199 | 64483090 |
| Gastric hypomotility | 17.00 | 14.44 | 4 | 9439 | 140 | 64489149 |
| Urinary tract infection | 16.97 | 14.44 | 73 | 9370 | 231523 | 64257766 |
| Acute kidney injury | 16.68 | 14.44 | 25 | 9418 | 449215 | 64040074 |
| Gait disturbance | 16.45 | 14.44 | 59 | 9384 | 172096 | 64317193 |
| Overdose | 16.38 | 14.44 | 56 | 9387 | 159510 | 64329779 |
| Developmental delay | 16.21 | 14.44 | 6 | 9437 | 1031 | 64488258 |
| Shunt malfunction | 15.08 | 14.44 | 4 | 9439 | 230 | 64489059 |
| Jaw disorder | 14.98 | 14.44 | 9 | 9434 | 4608 | 64484681 |
| Multiple sclerosis | 14.82 | 14.44 | 16 | 9427 | 18925 | 64470364 |
| Growth hormone-producing pituitary tumour | 14.72 | 14.44 | 3 | 9440 | 53 | 64489236 |
| Viral diarrhoea | 14.67 | 14.44 | 4 | 9439 | 255 | 64489034 |
| Multiple-drug resistance | 14.48 | 14.44 | 10 | 9433 | 6492 | 64482797 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N03AA03 | NERVOUS SYSTEM ANTIEPILEPTICS ANTIEPILEPTICS Barbiturates and derivatives |
| FDA PE | N0000008486 | Decreased Central Nervous System Disorganized Electrical Activity |
| MeSH PA | D000927 | Anticonvulsants |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D018682 | GABA Agents |
| MeSH PA | D018757 | GABA Modulators |
| MeSH PA | D018377 | Neurotransmitter Agents |
| CHEBI has role | CHEBI:35623 | anticonvulsants |
| CHEBI has role | CHEBI:35703 | Xenobiotic |
| CHEBI has role | CHEBI:78298 | environmental contaminants |
| FDA EPC | N0000175753 | Anti-epileptic Agent |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Tonic-clonic seizure | indication | 54200006 | |
| Epilepsy | indication | 84757009 | DOID:1826 |
| Bipolar disorder in remission | indication | 85248005 | |
| Localization-related epilepsy | indication | 230381009 | DOID:2234 |
| Lennox-Gastaut syndrome | indication | 230418006 | |
| Tonic-clonic epilepsy | indication | 352818000 | DOID:7725 |
| Epilepsy characterized by intractable complex partial seizures | indication | 442481002 | |
| Simple partial seizure | indication | 117891000119100 | |
| Bipolar affective disorder, current episode depression | off-label use | 191627008 | DOID:3312 |
| Neuropathic pain | off-label use | 247398009 | |
| Essential tremor | off-label use | 609558009 | DOID:4990 |
| Rapid Cycling Bipolar Affective Disorder | off-label use | ||
| Suicidal thoughts | contraindication | 6471006 | |
| Alcoholism | contraindication | 7200002 | |
| Constitutional aplastic anemia | contraindication | 28975000 | DOID:1342 |
| Depressive disorder | contraindication | 35489007 | |
| Megaloblastic anemia | contraindication | 53165003 | DOID:13382 |
| Acute nephropathy | contraindication | 58574008 | |
| Sleep apnea | contraindication | 73430006 | DOID:0050847 |
| Leukopenia | contraindication | 84828003 | DOID:615 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Pancytopenia | contraindication | 127034005 | DOID:12450 |
| Non-infective meningitis | contraindication | 230155003 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Anemia | contraindication | 271737000 | DOID:2355 |
| Pregnancy, function | contraindication | 289908002 | |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
| Aplastic anemia | contraindication | 306058006 | DOID:12449 |
| Granulocytopenic disorder | contraindication | 417672002 | |
| Porphyria | contraindication | 418470004 | |
| Primidone Toxicity | contraindication |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Dogs | Convulsions associated with idiopathic epilepsy | Indication |
| Dogs | Epileptiform convulsions | Indication |
| Dogs | Viral encephalitis | Indication |
| Dogs | Distemper | Indication |
| Dogs | Hardpad disease | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| Primidone | Zoetis Inc. | 1 |
| Mylepsin Tablets | Zoetis Inc. | 1 |
| Mylepsin, Primidone Medi-Pets | Zoetis Inc. | 1 |
| Neurosyn Tablets | Cronus Pharma Specialities India Private Limited | 1 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.99 | acidic |
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-1/beta-2/gamma-2 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | WOMBAT-PK | CHEMBL | |||||
| Transient receptor potential cation channel subfamily M member 3 | Ion channel | BLOCKER | IC50 | 6.20 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4018485 | VUID |
| N0000146807 | NUI |
| D00474 | KEGG_DRUG |
| 4018485 | VANDF |
| C0033148 | UMLSCUI |
| CHEBI:8412 | CHEBI |
| CHEMBL856 | ChEMBL_ID |
| DB00794 | DRUGBANK_ID |
| D011324 | MESH_DESCRIPTOR_UI |
| 4909 | PUBCHEM_CID |
| 248 | INN_ID |
| 5338 | IUPHAR_LIGAND_ID |
| 13AFD7670Q | UNII |
| 8691 | RXNORM |
| 390 | MMSL |
| 5355 | MMSL |
| d00352 | MMSL |
| 001626 | NDDF |
| 387256009 | SNOMEDCT_US |
| 47120002 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0527-1231 | TABLET | 250 mg | ORAL | ANDA | 14 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0527-1301 | TABLET | 50 mg | ORAL | ANDA | 14 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-5321 | TABLET | 250 mg | ORAL | ANDA | 13 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0615-8206 | TABLET | 50 mg | ORAL | ANDA | 11 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0904-5559 | TABLET | 50 mg | ORAL | ANDA | 14 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-522 | TABLET | 250 mg | ORAL | ANDA | 15 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-540 | TABLET | 50 mg | ORAL | ANDA | 15 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-509 | TABLET | 50 mg | ORAL | ANDA | 16 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-511 | TABLET | 250 mg | ORAL | ANDA | 16 sections |
| PRIMIDONE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42549-680 | TABLET | 50 mg | ORAL | ANDA | 14 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-1622 | TABLET | 250 mg | ORAL | ANDA | 13 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-4083 | TABLET | 250 mg | ORAL | ANDA | 12 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50268-686 | TABLET | 50 mg | ORAL | ANDA | 11 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50268-687 | TABLET | 250 mg | ORAL | ANDA | 11 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 53746-544 | TABLET | 50 mg | ORAL | ANDA | 12 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 53746-544 | TABLET | 50 mg | ORAL | ANDA | 12 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 53746-545 | TABLET | 250 mg | ORAL | ANDA | 12 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 53746-545 | TABLET | 250 mg | ORAL | ANDA | 12 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-1691 | TABLET | 250 mg | ORAL | ANDA | 14 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-5067 | TABLET | 50 mg | ORAL | ANDA | 14 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55111-476 | TABLET | 250 mg | ORAL | ANDA | 13 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55111-477 | TABLET | 50 mg | ORAL | ANDA | 13 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-7811 | TABLET | 50 mg | ORAL | ANDA | 12 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65162-544 | TABLET | 50 mg | ORAL | ANDA | 12 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65162-545 | TABLET | 250 mg | ORAL | ANDA | 12 sections |
| Mysoline | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66490-690 | TABLET | 50 mg | ORAL | NDA | 15 sections |
| Mysoline | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66490-691 | TABLET | 250 mg | ORAL | NDA | 15 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68084-202 | TABLET | 50 mg | ORAL | ANDA | 15 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68084-203 | TABLET | 250 mg | ORAL | ANDA | 15 sections |
| Primidone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68682-690 | TABLET | 250 mg | ORAL | NDA authorized generic | 15 sections |