betaxolol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| beta-adrenoreceptor antagonists | 356 | 63659-18-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A cardioselective beta-1-adrenergic antagonist with no partial agonist activity.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 20 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.45 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 15 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 2.17 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 85 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 4.80 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 3.40 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.40 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 17 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 30, 1985 | FDA | ALCON |
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 |
|---|---|---|---|---|---|---|
| Limb injury | 57.97 | 25.12 | 25 | 2335 | 20225 | 50582539 |
| Stevens-Johnson syndrome | 56.25 | 25.12 | 25 | 2335 | 21727 | 50581037 |
| Hyperaesthesia | 48.00 | 25.12 | 17 | 2343 | 8156 | 50594608 |
| Transient ischaemic attack | 46.92 | 25.12 | 25 | 2335 | 32185 | 50570579 |
| Fall | 46.75 | 25.12 | 67 | 2293 | 334865 | 50267899 |
| Angioplasty | 46.68 | 25.12 | 11 | 2349 | 1244 | 50601520 |
| Haemorrhage | 39.95 | 25.12 | 27 | 2333 | 53414 | 50549350 |
| Peripheral vascular disorder | 38.40 | 25.12 | 13 | 2347 | 5454 | 50597310 |
| Crepitations | 36.76 | 25.12 | 13 | 2347 | 6206 | 50596558 |
| Choking | 36.34 | 25.12 | 14 | 2346 | 8484 | 50594280 |
| Acquired haemophilia | 34.03 | 25.12 | 8 | 2352 | 895 | 50601869 |
| Bradycardia | 33.22 | 25.12 | 26 | 2334 | 64400 | 50538364 |
| Glaucoma | 31.09 | 25.12 | 15 | 2345 | 15671 | 50587093 |
| Status epilepticus | 30.19 | 25.12 | 14 | 2346 | 13392 | 50589372 |
| Fungal infection | 29.46 | 25.12 | 18 | 2342 | 29947 | 50572817 |
| Urinary retention | 29.04 | 25.12 | 17 | 2343 | 26173 | 50576591 |
| Asthma | 27.74 | 25.12 | 27 | 2333 | 89310 | 50513454 |
| Cardiac failure congestive | 27.13 | 25.12 | 26 | 2334 | 84356 | 50518408 |
| Sputum discoloured | 27.12 | 25.12 | 13 | 2347 | 13382 | 50589382 |
| Low density lipoprotein increased | 26.65 | 25.12 | 10 | 2350 | 5636 | 50597128 |
| Pulmonary congestion | 25.52 | 25.12 | 13 | 2347 | 15234 | 50587530 |
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 |
|---|---|---|---|---|---|---|
| Wrong drug | 41.01 | 26.56 | 6 | 823 | 79 | 29573619 |
| Splenic rupture | 34.36 | 26.56 | 8 | 821 | 1438 | 29572260 |
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 |
|---|---|---|---|---|---|---|
| Limb injury | 63.06 | 20.60 | 28 | 3081 | 23477 | 64472146 |
| Fall | 54.04 | 20.60 | 82 | 3027 | 416744 | 64078879 |
| Transient ischaemic attack | 48.98 | 20.60 | 29 | 3080 | 44153 | 64451470 |
| Angioplasty | 48.05 | 20.60 | 12 | 3097 | 1673 | 64493950 |
| Haemorrhage | 44.26 | 20.60 | 34 | 3075 | 79317 | 64416306 |
| Hyperaesthesia | 44.07 | 20.60 | 17 | 3092 | 9997 | 64485626 |
| Peripheral vascular disorder | 38.02 | 20.60 | 14 | 3095 | 7247 | 64488376 |
| Crepitations | 36.85 | 20.60 | 14 | 3095 | 7901 | 64487722 |
| Wound | 36.70 | 20.60 | 30 | 3079 | 76447 | 64419176 |
| Bradycardia | 36.21 | 20.60 | 36 | 3073 | 118183 | 64377440 |
| Choking | 32.97 | 20.60 | 14 | 3095 | 10524 | 64485099 |
| Wrong drug | 31.58 | 20.60 | 6 | 3103 | 232 | 64495391 |
| Asthma | 31.01 | 20.60 | 30 | 3079 | 95195 | 64400428 |
| Glaucoma | 30.02 | 20.60 | 15 | 3094 | 16333 | 64479290 |
| Acquired haemophilia | 29.12 | 20.60 | 8 | 3101 | 1612 | 64494011 |
| Sputum discoloured | 28.76 | 20.60 | 15 | 3094 | 17841 | 64477782 |
| Fungal infection | 26.70 | 20.60 | 18 | 3091 | 34233 | 64461390 |
| Splenic rupture | 26.64 | 20.60 | 8 | 3101 | 2211 | 64493412 |
| Low density lipoprotein increased | 23.27 | 20.60 | 10 | 3099 | 7730 | 64487893 |
| Cardiac failure congestive | 23.23 | 20.60 | 30 | 3079 | 130550 | 64365073 |
| Pulmonary congestion | 22.16 | 20.60 | 14 | 3095 | 23866 | 64471757 |
| Urinary retention | 20.89 | 20.60 | 18 | 3091 | 49183 | 64446440 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C07AB05 | CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Beta blocking agents, selective |
| ATC | S01ED02 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIGLAUCOMA PREPARATIONS AND MIOTICS Beta blocking agents |
| ATC | S01ED52 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIGLAUCOMA PREPARATIONS AND MIOTICS Beta blocking agents |
| FDA MoA | N0000000161 | Adrenergic beta-Antagonists |
| FDA EPC | N0000175556 | beta-Adrenergic Blocker |
| CHEBI has role | CHEBI:35530 | beta-adrenergic blockers |
| CHEBI has role | CHEBI:35674 | antihypertensive drugs |
| CHEBI has role | CHEBI:66991 | sympatholytic drug |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D018674 | Adrenergic Antagonists |
| MeSH PA | D058671 | Adrenergic beta-1 Receptor Antagonists |
| MeSH PA | D000319 | Adrenergic beta-Antagonists |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D013565 | Sympatholytics |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Ocular hypertension | indication | 4210003 | DOID:9282 |
| Hypertensive disorder | indication | 38341003 | DOID:10763 |
| Open-angle glaucoma | indication | 84494001 | DOID:1067 |
| Malignant glaucoma | off-label use | 10100008 | |
| Aphakic glaucoma | off-label use | 15374009 | |
| Secondary glaucoma | off-label use | 95717004 | |
| Bronchospasm | contraindication | 4386001 | |
| Psoriasis | contraindication | 9014002 | DOID:8893 |
| Complete atrioventricular block | contraindication | 27885002 | |
| Acute cerebrovascular insufficiency | contraindication | 29322000 | |
| Depressive disorder | contraindication | 35489007 | |
| Anaphylaxis | contraindication | 39579001 | |
| Chronic heart failure | contraindication | 48447003 | |
| Sinus bradycardia | contraindication | 49710005 | |
| Acute nephropathy | contraindication | 58574008 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Pulmonary emphysema | contraindication | 87433001 | |
| Cardiogenic shock | contraindication | 89138009 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Myasthenia gravis | contraindication | 91637004 | DOID:437 |
| Second degree atrioventricular block | contraindication | 195042002 | |
| Decompensated cardiac failure | contraindication | 195111005 | |
| Asthma | contraindication | 195967001 | DOID:2841 |
| Heart block | contraindication | 233916004 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Hypoglycemic disorder | contraindication | 237630007 | |
| Raynaud's phenomenon | contraindication | 266261006 | |
| Pregnancy, function | contraindication | 289908002 | |
| Pheochromocytoma | contraindication | 302835009 | |
| 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 | 9.19 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Beta-1 adrenergic receptor | GPCR | ANTAGONIST | Kd | 8.80 | WOMBAT-PK | CHEMBL | |||
| Beta-2 adrenergic receptor | GPCR | Kd | 7.20 | WOMBAT-PK | |||||
| Beta-2 adrenergic receptor | GPCR | Kd | 6.98 | CHEMBL | |||||
| Beta-2 adrenergic receptor | GPCR | IC50 | 6.18 | CHEMBL | |||||
| Beta-1 adrenergic receptor | GPCR | Kd | 8.53 | CHEMBL | |||||
| Beta-1 adrenergic receptor | GPCR | Kd | 8.76 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019633 | VUID |
| N0000147726 | NUI |
| D00598 | KEGG_DRUG |
| 63659-19-8 | SECONDARY_CAS_RN |
| 142144 | RXNORM |
| C0005320 | UMLSCUI |
| CHEBI:3082 | CHEBI |
| CHEMBL423 | ChEMBL_ID |
| CHEMBL1691 | ChEMBL_ID |
| DB00195 | DRUGBANK_ID |
| D015784 | MESH_DESCRIPTOR_UI |
| 2369 | PUBCHEM_CID |
| 549 | IUPHAR_LIGAND_ID |
| 4530 | INN_ID |
| O0ZR1R6RZ2 | UNII |
| 31545 | MMSL |
| 4280 | MMSL |
| d00176 | MMSL |
| 001859 | NDDF |
| 004743 | NDDF |
| 349900007 | SNOMEDCT_US |
| 387195001 | SNOMEDCT_US |
| 409276006 | SNOMEDCT_US |
| 4018588 | VANDF |
| 4019633 | VANDF |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Betoptic S | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0065-0246 | SUSPENSION/ DROPS | 2.80 mg | OPHTHALMIC | NDA | 25 sections |
| Betaxolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-623 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 19 sections |
| Betaxolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-624 | TABLET, FILM COATED | 20 mg | ORAL | ANDA | 19 sections |
| BETAXOLOL HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10702-013 | TABLET, COATED | 10 mg | ORAL | ANDA | 12 sections |
| BETAXOLOL HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10702-014 | TABLET, COATED | 20 mg | ORAL | ANDA | 12 sections |
| Betaxolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-705 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 19 sections |
| Betaxolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-705 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 19 sections |
| Betaxolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24658-700 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 17 sections |
| Betaxolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24658-701 | TABLET, FILM COATED | 20 mg | ORAL | ANDA | 17 sections |
| Betaxolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42806-038 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 17 sections |
| Betaxolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42806-039 | TABLET, FILM COATED | 20 mg | ORAL | ANDA | 17 sections |
| Betaxolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-4932 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 17 sections |
| Betaxolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60429-753 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 12 sections |
| Betaxolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60429-754 | TABLET, FILM COATED | 20 mg | ORAL | ANDA | 12 sections |
| Betaxolol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61314-245 | SOLUTION/ DROPS | 5.60 mg | OPHTHALMIC | NDA authorized generic | 19 sections |