butalbital 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| hypnotics, barbituric acid derivatives | 441 | 77-26-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
management of butalbital withdrawal can be simplified by using a phenobarbital-loading protocol; RN given refers to parent cpd
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 |
| EoM (Fraction excreted unchanged in urine) | 3.60 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 22.30 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 85 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 4, 1976 | FDA | ACTAVIS LABS UT 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 |
|---|---|---|---|---|---|---|
| Completed suicide | 230.89 | 15.14 | 160 | 6580 | 145513 | 63336769 |
| Death | 139.28 | 15.14 | 184 | 6556 | 374197 | 63108085 |
| Toxicity to various agents | 77.30 | 15.14 | 112 | 6628 | 247138 | 63235144 |
| Migraine | 51.40 | 15.14 | 59 | 6681 | 103287 | 63378995 |
| Cholecystitis chronic | 48.06 | 15.14 | 23 | 6717 | 10338 | 63471944 |
| Drug abuse | 38.76 | 15.14 | 43 | 6697 | 72475 | 63409807 |
| Cardio-respiratory arrest | 31.08 | 15.14 | 35 | 6705 | 59924 | 63422358 |
| Peritoneal perforation | 30.65 | 15.14 | 6 | 6734 | 120 | 63482162 |
| Poisoning | 28.76 | 15.14 | 18 | 6722 | 13682 | 63468600 |
| Headache | 25.99 | 15.14 | 134 | 6606 | 633107 | 62849175 |
| Hypoaesthesia | 24.79 | 15.14 | 55 | 6685 | 168338 | 63313944 |
| Product complaint | 22.38 | 15.14 | 15 | 6725 | 12794 | 63469488 |
| Breast cyst | 21.98 | 15.14 | 8 | 6732 | 1813 | 63480469 |
| Drug abuser | 21.62 | 15.14 | 9 | 6731 | 2914 | 63479368 |
| Injection site necrosis | 20.40 | 15.14 | 7 | 6733 | 1337 | 63480945 |
| Emotional distress | 20.38 | 15.14 | 21 | 6719 | 32528 | 63449754 |
| Tracheitis | 19.58 | 15.14 | 6 | 6734 | 801 | 63481481 |
| Depression | 18.31 | 15.14 | 54 | 6686 | 196438 | 63285844 |
| Intentional product misuse | 18.09 | 15.14 | 27 | 6713 | 60890 | 63421392 |
| Dependence | 17.43 | 15.14 | 7 | 6733 | 2070 | 63480212 |
| Gallbladder disorder | 17.23 | 15.14 | 15 | 6725 | 18827 | 63463455 |
| Anxiety | 15.90 | 15.14 | 55 | 6685 | 217486 | 63264796 |
| Injury | 15.68 | 15.14 | 28 | 6712 | 73219 | 63409063 |
| Off label use | 15.63 | 15.14 | 30 | 6710 | 674432 | 62807850 |
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 |
|---|---|---|---|---|---|---|
| Death | 89.52 | 26.03 | 78 | 870 | 397971 | 34558012 |
| Cardio-respiratory arrest | 44.33 | 26.03 | 24 | 924 | 55249 | 34900734 |
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 |
|---|---|---|---|---|---|---|
| Death | 267.04 | 17.25 | 253 | 5145 | 566261 | 79172729 |
| Completed suicide | 262.98 | 17.25 | 178 | 5220 | 245589 | 79493401 |
| Toxicity to various agents | 101.28 | 17.25 | 133 | 5265 | 421407 | 79317583 |
| Cardio-respiratory arrest | 71.52 | 17.25 | 59 | 5339 | 108451 | 79630539 |
| Drug abuse | 51.26 | 17.25 | 59 | 5339 | 162632 | 79576358 |
| Migraine | 48.30 | 17.25 | 43 | 5355 | 87450 | 79651540 |
| Cholecystitis chronic | 45.24 | 17.25 | 19 | 5379 | 9887 | 79729103 |
| Peritoneal perforation | 31.35 | 17.25 | 6 | 5392 | 170 | 79738820 |
| Poisoning | 28.48 | 17.25 | 19 | 5379 | 25253 | 79713737 |
| Emotional distress | 26.85 | 17.25 | 22 | 5376 | 39947 | 79699043 |
| Off label use | 25.47 | 17.25 | 15 | 5383 | 907200 | 78831790 |
| Injection site necrosis | 22.84 | 17.25 | 7 | 5391 | 1471 | 79737519 |
| Drug abuser | 22.43 | 17.25 | 10 | 5388 | 6003 | 79732987 |
| Headache | 22.07 | 17.25 | 95 | 5303 | 653677 | 79085313 |
| Injury | 20.90 | 17.25 | 26 | 5372 | 77470 | 79661520 |
| Gallbladder disorder | 20.50 | 17.25 | 14 | 5384 | 19326 | 79719664 |
| Dependence | 19.45 | 17.25 | 7 | 5391 | 2415 | 79736575 |
| Tracheitis | 19.30 | 17.25 | 6 | 5392 | 1322 | 79737668 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| FDA CS | M0002177 | Barbiturates |
| FDA EPC | N0000175693 | Barbiturate |
| CHEBI has role | CHEBI:35717 | hypnotics |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Tension-type headache | indication | 398057008 | |
| Migraine | off-label use | 37796009 | DOID:6364 |
| Necrotizing enterocolitis in fetus OR newborn | contraindication | 2707005 | |
| Suicidal thoughts | contraindication | 6471006 | |
| Dependent drug abuse | contraindication | 6525002 | |
| Alcoholism | contraindication | 7200002 | |
| Hyperammonemia | contraindication | 9360008 | |
| Peptic ulcer | contraindication | 13200003 | DOID:750 |
| Chronic obstructive lung disease | contraindication | 13645005 | DOID:3083 |
| Hepatic encephalopathy | contraindication | 13920009 | DOID:13413 |
| Chronic disease of respiratory system | contraindication | 17097001 | |
| Mood swings | contraindication | 18963009 | |
| Inflammatory bowel disease | contraindication | 24526004 | DOID:0050589 |
| Depressive disorder | contraindication | 35489007 | |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Disorder of gallbladder | contraindication | 39621005 | DOID:0060262 |
| Gastrointestinal ulcer | contraindication | 40845000 | |
| Hypothyroidism | contraindication | 40930008 | DOID:1459 |
| Hyperactive behavior | contraindication | 44548000 | |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Low blood pressure | contraindication | 45007003 | |
| Bradycardia | contraindication | 48867003 | |
| Vitamin K deficiency | contraindication | 52675005 | DOID:11249 |
| Nasal polyp | contraindication | 52756005 | |
| Acute nephropathy | contraindication | 58574008 | |
| Hepatic failure | contraindication | 59927004 | |
| Drug AND/OR toxin-induced diarrhea | contraindication | 65979008 | |
| Substance abuse | contraindication | 66214007 | |
| Benign intracranial hypertension | contraindication | 68267002 | DOID:11459 |
| Poisoning by acetaminophen | contraindication | 70273001 | |
| Agoraphobia | contraindication | 70691001 | DOID:593 |
| Hepatic coma | contraindication | 72836002 | DOID:12550 |
| Sleep apnea | contraindication | 73430006 | DOID:0050847 |
| Factor II deficiency | contraindication | 73975000 | |
| Reye's syndrome | contraindication | 74351001 | DOID:14525 |
| Gastrointestinal hemorrhage | contraindication | 74474003 | |
| Urethral stricture | contraindication | 76618002 | |
| Thrombotic thrombocytopenic purpura | contraindication | 78129009 | DOID:10772 |
| Decreased respiratory function | contraindication | 80954004 | |
| Injury of head | contraindication | 82271004 | |
| Epilepsy | contraindication | 84757009 | DOID:1826 |
| Gout | contraindication | 90560007 | DOID:13189 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Hemophilia | contraindication | 90935002 | |
| Anemia due to enzyme deficiency | contraindication | 111577008 | |
| Acute abdominal pain | contraindication | 116290004 | |
| Procedure on urinary system | contraindication | 118677009 | |
| von Willebrand disorder | contraindication | 128105004 | DOID:12531 |
| Seizure disorder | contraindication | 128613002 | |
| Obsessive-compulsive disorder | contraindication | 191736004 | DOID:10933 |
| Insomnia | contraindication | 193462001 | |
| Impaired renal function disorder | contraindication | 197663003 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Sleep automatism | contraindication | 247962006 | |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Anemia | contraindication | 271737000 | DOID:2355 |
| Pregnancy, function | contraindication | 289908002 | |
| Lesion of brain | contraindication | 301766008 | |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
| Panic disorder | contraindication | 371631005 | DOID:594 |
| Primary adrenocortical insufficiency | contraindication | 373662000 | |
| Operation on gastrointestinal tract | contraindication | 386621005 | |
| Pseudomembranous enterocolitis | contraindication | 397683000 | |
| Respiratory insufficiency | contraindication | 409623005 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Myocardial ischemia | contraindication | 414795007 | DOID:3393 |
| Myocardial infarction in recovery phase | contraindication | 418044006 | |
| Central nervous system depression | contraindication | 418072004 | |
| Porphyria | contraindication | 418470004 | |
| Ultrarapid metabolizer due to cytochrome p450 CYP2D6 variant | contraindication | 422681000 | |
| Dysfunction of sphincter of Oddi | contraindication | 430887001 | |
| Acute erosive gastritis | contraindication | 444926003 | |
| Acute exacerbation of asthma | contraindication | 708038006 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.65 | acidic |
| pKa2 | 9.34 | 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-3/gamma-2 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | WOMBAT-PK | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4018107 | VUID |
| N0000179058 | NUI |
| D03182 | KEGG_DRUG |
| 19860 | RXNORM |
| C0054234 | UMLSCUI |
| CHEBI:102524 | CHEBI |
| CHEMBL454 | ChEMBL_ID |
| DB00241 | DRUGBANK_ID |
| 2481 | PUBCHEM_CID |
| C004470 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7138 | IUPHAR_LIGAND_ID |
| 7 | INN_ID |
| KHS0AZ4JVK | UNII |
| 4311 | MMSL |
| 72849 | MMSL |
| d03061 | MMSL |
| 387563005 | SNOMEDCT_US |
| 96196008 | SNOMEDCT_US |
| 4018107 | VANDF |
| 001423 | NDDF |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Fiorinal with Codeine | HUMAN PRESCRIPTION DRUG LABEL | 4 | 0023-6010 | CAPSULE | 50 mg | ORAL | NDA | 36 sections |
| Fiorinal | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0023-6146 | CAPSULE | 50 mg | ORAL | NDA | 23 sections |
| Butalbital, Acetaminophen, Caffeine and Codeine Phosphate | HUMAN PRESCRIPTION DRUG LABEL | 4 | 0054-0650 | CAPSULE | 50 mg | ORAL | ANDA | 33 sections |
| Butalbital, Acetaminophen, Caffeine and Codeine Phosphate | HUMAN PRESCRIPTION DRUG LABEL | 4 | 0054-0650 | CAPSULE | 50 mg | ORAL | ANDA | 33 sections |
| Butalbital, Acetaminophen, Caffeine and Codeine Phosphate | HUMAN PRESCRIPTION DRUG LABEL | 4 | 0054-3000 | CAPSULE | 50 mg | ORAL | ANDA | 33 sections |
| Butalbital, Acetaminophen, Caffeine and Codeine Phosphate | HUMAN PRESCRIPTION DRUG LABEL | 4 | 0054-3000 | CAPSULE | 50 mg | ORAL | ANDA | 33 sections |
| BUPAP | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0095-3000 | TABLET | 50 mg | ORAL | ANDA | 25 sections |
| Butalbital, Acetaminophen, and Caffeine | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0143-0170 | CAPSULE | 50 mg | ORAL | ANDA | 26 sections |
| Butalbital, Aspirin, Caffeine and Codeine Phosphate | HUMAN PRESCRIPTION DRUG LABEL | 4 | 0527-1312 | CAPSULE | 50 mg | ORAL | ANDA | 25 sections |
| Butalbital, aspirin, and caffeine | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0527-1552 | CAPSULE | 50 mg | ORAL | ANDA | 25 sections |
| Butalbital, aspirin, and caffeine | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0527-1552 | CAPSULE | 50 mg | ORAL | ANDA | 25 sections |
| Butalbital, Acetaminophen, and Caffeine | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0527-1695 | TABLET | 50 mg | ORAL | ANDA | 27 sections |
| Butalbital, Acetaminophen, and Caffeine | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0527-1695 | TABLET | 50 mg | ORAL | ANDA | 27 sections |
| butalbital, acetaminophen and caffeine | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0527-4094 | CAPSULE | 50 mg | ORAL | ANDA | 27 sections |
| butalbital, acetaminophen and caffeine | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0527-4094 | CAPSULE | 50 mg | ORAL | ANDA | 27 sections |
| Butalbital, Acetaminophen, and Caffeine | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0527-4095 | CAPSULE | 50 mg | ORAL | ANDA | 27 sections |
| Butalbital, Acetaminophen, and Caffeine | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0527-4095 | CAPSULE | 50 mg | ORAL | ANDA | 27 sections |
| Butalbital, Acetaminophen, and Caffeine | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0591-2640 | CAPSULE | 50 mg | ORAL | ANDA | 25 sections |
| Butalbital, Acetaminophen, and Caffeine | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0591-2640 | CAPSULE | 50 mg | ORAL | ANDA | 25 sections |
| Butalbital, Acetaminophen, Caffeine, and Codeine Phosphate | HUMAN PRESCRIPTION DRUG LABEL | 4 | 0591-2641 | CAPSULE | 50 mg | ORAL | ANDA | 27 sections |
| Butalbital, Aspirin, and Caffeine | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0591-3219 | CAPSULE | 50 mg | ORAL | NDA authorized generic | 24 sections |
| Butalbital, Acetaminophen, Caffeine, and Codeine Phosphate | HUMAN PRESCRIPTION DRUG LABEL | 4 | 0591-3220 | CAPSULE | 50 mg | ORAL | NDA AUTHORIZED GENERIC | 32 sections |
| Butalbital, Acetaminophen, Caffeine, and Codeine Phosphate | HUMAN PRESCRIPTION DRUG LABEL | 4 | 0591-3220 | CAPSULE | 50 mg | ORAL | NDA AUTHORIZED GENERIC | 32 sections |
| Butalbital, Acetaminophen, Caffeine, and Codeine Phosphate | HUMAN PRESCRIPTION DRUG LABEL | 4 | 0591-3220 | CAPSULE | 50 mg | ORAL | NDA AUTHORIZED GENERIC | 32 sections |
| Butalbital, Acetaminophen, and Caffeine | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0591-3369 | TABLET | 50 mg | ORAL | ANDA | 27 sections |
| Butalbital, Aspirin, Caffeine and Codeine Phosphate | HUMAN PRESCRIPTION DRUG LABEL | 4 | 0591-3546 | CAPSULE | 50 mg | ORAL | NDA authorized generic | 38 sections |
| butalbital and acetaminophen | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0603-2540 | TABLET | 50 mg | ORAL | ANDA | 25 sections |
| butalbital and acetaminophen | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0603-2540 | TABLET | 50 mg | ORAL | ANDA | 25 sections |
| Butalbital, Acetaminophen and Caffeine | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0603-2544 | TABLET | 50 mg | ORAL | ANDA | 27 sections |
| Butalbital, Acetaminophen and Caffeine | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0603-2544 | TABLET | 50 mg | ORAL | ANDA | 27 sections |