betaxolol 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 |
|---|---|---|---|---|---|---|
| Stevens-Johnson syndrome | 50.70 | 25.43 | 24 | 2229 | 23273 | 46660536 |
| Limb injury | 48.74 | 25.43 | 22 | 2231 | 19152 | 46664657 |
| Fall | 45.92 | 25.43 | 67 | 2186 | 329030 | 46354779 |
| Hyperaesthesia | 40.60 | 25.43 | 15 | 2238 | 7841 | 46675968 |
| Transient ischaemic attack | 36.31 | 25.43 | 22 | 2231 | 34881 | 46648928 |
| Wound | 34.60 | 25.43 | 23 | 2230 | 42779 | 46641030 |
| Bradycardia | 33.91 | 25.43 | 27 | 2226 | 66271 | 46617538 |
| Acquired haemophilia | 33.52 | 25.43 | 8 | 2245 | 923 | 46682886 |
| Haemorrhage | 31.65 | 25.43 | 24 | 2229 | 54845 | 46628964 |
| Status epilepticus | 29.17 | 25.43 | 14 | 2239 | 13965 | 46669844 |
| Glaucoma | 27.44 | 25.43 | 14 | 2239 | 15907 | 46667902 |
| Angioplasty | 26.26 | 25.43 | 7 | 2246 | 1260 | 46682549 |
| Choking | 25.77 | 25.43 | 11 | 2242 | 8365 | 46675444 |
| Peripheral vascular disorder | 25.77 | 25.43 | 10 | 2243 | 5967 | 46677842 |
| Low density lipoprotein increased | 25.73 | 25.43 | 10 | 2243 | 5990 | 46677819 |
| Crepitations | 25.58 | 25.43 | 10 | 2243 | 6082 | 46677727 |
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 | 42.12 | 26.48 | 6 | 807 | 67 | 29951598 |
| Splenic rupture | 34.14 | 26.48 | 8 | 805 | 1528 | 29950137 |
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-adrenoceptor antagonists |
| CHEBI has role | CHEBI:35674 | antihypertensive |
| CHEBI has role | CHEBI:66991 | sympatholytics |
| 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 (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 |
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 | IC50 | 6.18 | CHEMBL | |||||
| Beta-2 adrenergic receptor | GPCR | Kd | 6.98 | CHEMBL | |||||
| Beta-1 adrenergic receptor | GPCR | Kd | 8.76 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| O0ZR1R6RZ2 | UNII |
| 4019633 | VUID |
| N0000147726 | NUI |
| D00598 | KEGG_DRUG |
| 63659-19-8 | SECONDARY_CAS_RN |
| 4018588 | VANDF |
| 4019633 | VANDF |
| C0005320 | UMLSCUI |
| CHEBI:3082 | CHEBI |
| CHEMBL423 | ChEMBL_ID |
| CHEMBL1691 | ChEMBL_ID |
| DB00195 | DRUGBANK_ID |
| D015784 | MESH_DESCRIPTOR_UI |
| 4530 | INN_ID |
| 2369 | PUBCHEM_CID |
| 549 | IUPHAR_LIGAND_ID |
| 142144 | RXNORM |
| 31545 | MMSL |
| 4280 | MMSL |
| d00176 | MMSL |
| 001859 | NDDF |
| 004743 | NDDF |
| 349900007 | SNOMEDCT_US |
| 387195001 | SNOMEDCT_US |
| 409276006 | SNOMEDCT_US |
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 | 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 | 60429-753 | 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 | 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 |