levobunolol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| beta-adrenoreceptor antagonists | 431 | 47141-42-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
The L-Isomer of bunolol.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 75 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 19, 1985 | FDA | ALLERGAN |
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 |
|---|---|---|---|---|---|---|
| Floppy iris syndrome | 43.32 | 37.40 | 5 | 163 | 117 | 63488737 |
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | S01ED03 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIGLAUCOMA PREPARATIONS AND MIOTICS Beta blocking agents |
| FDA MoA | N0000000161 | Adrenergic beta-Antagonists |
| FDA EPC | N0000175556 | beta-Adrenergic Blocker |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D018674 | Adrenergic Antagonists |
| MeSH PA | D000319 | Adrenergic beta-Antagonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D013565 | Sympatholytics |
| CHEBI has role | CHEBI:35530 | beta-adrenergic blockers |
| CHEBI has role | CHEBI:39456 | antiglaucoma agent |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Ocular hypertension | indication | 4210003 | DOID:9282 |
| Open-angle glaucoma | indication | 84494001 | DOID:1067 |
| Complete atrioventricular block | contraindication | 27885002 | |
| Acute cerebrovascular insufficiency | contraindication | 29322000 | |
| Anaphylaxis | contraindication | 39579001 | |
| Sinus bradycardia | contraindication | 49710005 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Pulmonary emphysema | contraindication | 87433001 | |
| Cardiogenic shock | contraindication | 89138009 | |
| Myasthenia gravis | contraindication | 91637004 | DOID:437 |
| Second degree atrioventricular block | contraindication | 195042002 | |
| Decompensated cardiac failure | contraindication | 195111005 | |
| Asthma | contraindication | 195967001 | DOID:2841 |
| Pregnancy, function | contraindication | 289908002 | |
| Severe chronic obstructive pulmonary disease | contraindication | 313299006 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.31 | 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 | Ki | 8.40 | DRUG MATRIX | CHEMBL | |||
| Beta-2 adrenergic receptor | GPCR | ANTAGONIST | Ki | 9.26 | DRUG MATRIX | CHEMBL | |||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 6.49 | DRUG MATRIX | |||||
| Sodium-dependent serotonin transporter | Transporter | Ki | 5.59 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 5.78 | DRUG MATRIX | |||||
| Beta-3 adrenergic receptor | GPCR | ANTAGONIST | Ki | 6.59 | DRUG MATRIX | ||||
| 5-hydroxytryptamine receptor 1A | GPCR | IC50 | 5.54 | CHEMBL | |||||
| Beta-3 adrenergic receptor | GPCR | ANTAGONIST | Ki | 6.30 | IUPHAR | ||||
| Beta-3 adrenergic receptor | GPCR | ANTAGONIST | Ki | 6.40 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4019799 | VUID |
| N0000147888 | NUI |
| D01025 | KEGG_DRUG |
| 27912-14-7 | SECONDARY_CAS_RN |
| 151434 | RXNORM |
| C0006388 | UMLSCUI |
| CHEBI:6438 | CHEBI |
| CHEMBL1201237 | ChEMBL_ID |
| DB01210 | DRUGBANK_ID |
| CHEMBL1201177 | ChEMBL_ID |
| D002040 | MESH_DESCRIPTOR_UI |
| 39468 | PUBCHEM_CID |
| 570 | IUPHAR_LIGAND_ID |
| 4706 | INN_ID |
| G6317AOI7K | UNII |
| 263 | MMSL |
| 4968 | MMSL |
| 7927 | MMSL |
| 349903009 | SNOMEDCT_US |
| 387349000 | SNOMEDCT_US |
| 418934007 | SNOMEDCT_US |
| 4019151 | VANDF |
| 4019799 | VANDF |
| 001860 | NDDF |
| 004744 | NDDF |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| BETAGAN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0023-4385 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | NDA | 19 sections |
| Levobunolol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24208-505 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 19 sections |
| Levobunolol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24208-505 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 19 sections |
| Levobunolol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-3363 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 17 sections |