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pindolol ๐ถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| beta-adrenoreceptor antagonists | 2176 | 13523-86-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 15 | mg | O |
| 15 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 4.03 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Hosey CM, Chan R, Benet LZ |
| S (Water solubility) | 0.86 mg/mL | Bocci G, Oprea TI, Benet LZ |
| EoM (Fraction excreted unchanged in urine) | 54 % | Hosey CM, Chan R, Benet LZ |
| BA (Bioavailability) | 88 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 1.20 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 7.70 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.58 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 2.20 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,IKBKB,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 | 54 | |||
| kinase-selectivity-class | AXL,BRAF,CAMK2D,CDK4,CDK9,DDR1,DYRK1B,MAP3K10,MAP3K21,MAPK7,PIK3CB,PIK3CD,PRKCD,SIK2,STK33 | 15 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 1.824 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | Moderate | 0.66 | |
| rat-kpuu-brain | Rat brain Kpuu | 0.166 | % | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 3, 1982 | FDA |
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 |
|---|---|---|---|---|---|---|
| Atrioventricular block complete | 114.96 | 35.31 | 24 | 668 | 9787 | 90617968 |
| Oesophagitis | 70.88 | 35.31 | 18 | 674 | 17231 | 90610524 |
| White blood cell count abnormal | 63.18 | 35.31 | 14 | 678 | 7490 | 90620265 |
| Neutrophil count abnormal | 59.44 | 35.31 | 12 | 680 | 4116 | 90623639 |
| Rhabdomyolysis | 55.41 | 35.31 | 19 | 673 | 51237 | 90576518 |
| Urinary tract infection | 54.77 | 35.31 | 32 | 660 | 305600 | 90322155 |
| Haemoglobin abnormal | 52.96 | 35.31 | 12 | 680 | 7088 | 90620667 |
| Drug interaction | 39.29 | 35.31 | 25 | 667 | 276428 | 90351327 |
| Hypertension | 38.52 | 35.31 | 30 | 662 | 457502 | 90170253 |
| Chromaturia | 36.74 | 35.31 | 11 | 681 | 19176 | 90608579 |
FDA Adverse Event Reporting System (Male)
None
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 |
|---|---|---|---|---|---|---|
| Atrioventricular block complete | 100.45 | 32.22 | 24 | 732 | 20058 | 110568485 |
| Rhabdomyolysis | 41.69 | 32.22 | 19 | 737 | 120382 | 110468161 |
| Hypertension | 36.35 | 32.22 | 29 | 727 | 510055 | 110078488 |
| Chromaturia | 33.32 | 32.22 | 11 | 745 | 29349 | 110559194 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C07AA03 | CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Beta blocking agents, non-selective |
| ATC | C07CA03 | CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS AND OTHER DIURETICS Beta blocking agents, non-selective, and other diuretics |
| FDA MoA | N0000000161 | Adrenergic beta-Antagonists |
| FDA EPC | N0000175556 | beta-Adrenergic Blocker |
| MeSH PA | D000319 | Adrenergic beta-Antagonists |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D012702 | Serotonin Antagonists |
| MeSH PA | D014665 | Vasodilator Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018490 | Serotonin Agents |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D018674 | Adrenergic Antagonists |
| CHEBI has role | CHEBI:35469 | antidepressant |
| CHEBI has role | CHEBI:35530 | ฮฒ-adrenergic antagonist |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
| CHEBI has role | CHEBI:35620 | vasodilator agent |
| CHEBI has role | CHEBI:35674 | antihypertensive agent |
| CHEBI has role | CHEBI:39456 | antiglaucoma drug |
| CHEBI has role | CHEBI:48279 | serotonergic antagonist |
Related Drugs by ATC class:
C07AA Beta blocking agents, non-selective 13 drugs
C07CA Beta blocking agents, non-selective, and other diuretics 3 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypertensive disorder | indication | 38341003 | DOID:10763 |
| Angina pectoris | off-label use | 194828000 | |
| Bronchospasm | contraindication | 4386001 | |
| Complete atrioventricular block | contraindication | 27885002 | |
| Depressive disorder | contraindication | 35489007 | |
| Anaphylaxis | contraindication | 39579001 | |
| Sinus bradycardia | contraindication | 49710005 | |
| 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 |
| Partial atrioventricular block | contraindication | 195039008 | |
| Decompensated cardiac failure | contraindication | 195111005 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Raynaud's phenomenon | contraindication | 266261006 | |
| Pregnancy, function | contraindication | 289908002 | |
| Severe chronic obstructive pulmonary disease | contraindication | 313299006 | |
| Right ventricular failure | contraindication | 367363000 |
๐ถ Veterinary Drug Use
None
๐ถ Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.41 | acidic |
| pKa2 | 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 | PARTIAL AGONIST | Ki | 9.40 | WOMBAT-PK | CHEMBL | |||
| Beta-2 adrenergic receptor | GPCR | PARTIAL AGONIST | Ki | 9 | WOMBAT-PK | CHEMBL | |||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 8.10 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | AGONIST | Ki | 5 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 2B | GPCR | AGONIST | Ki | 5.70 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 4.27 | CHEMBL | |||||
| D(3) dopamine receptor | GPCR | Ki | 6 | CHEMBL | |||||
| Beta-3 adrenergic receptor | GPCR | Kd | 6.78 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1B | GPCR | Ki | 7.10 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 1D | GPCR | Ki | 5.21 | PDSP | |||||
| D(4) dopamine receptor | GPCR | Ki | 5.78 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 5A | GPCR | Ki | 5.15 | CHEMBL | |||||
| Transmembrane protein 97 | Enzyme | Ki | 5.48 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1B | GPCR | Ki | 7.10 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 7.70 | CHEMBL | |||||
| Serotonin 1 (5-HT1) receptor | GPCR | Ki | 7 | CHEMBL | |||||
| Serotonin 2 (5-HT2) receptor | GPCR | Ki | 4.53 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4018760 | VUID |
| N0000147063 | NUI |
| D00513 | KEGG_DRUG |
| 4018760 | VANDF |
| C0031937 | UMLSCUI |
| CHEBI:8214 | CHEBI |
| CHEMBL500 | ChEMBL_ID |
| DB00960 | DRUGBANK_ID |
| D010869 | MESH_DESCRIPTOR_UI |
| 4828 | PUBCHEM_CID |
| 91 | IUPHAR_LIGAND_ID |
| 2698 | INN_ID |
| BJ4HF6IU1D | UNII |
| 8332 | RXNORM |
| 1482 | MMSL |
| 5302 | MMSL |
| d00137 | MMSL |
| 001857 | NDDF |
| 18381001 | SNOMEDCT_US |
| 387102009 | SNOMEDCT_US |
| BJ4HF6IU1D | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-743 | TABLET | 5 mg | ORAL | ANDA | 19 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-744 | TABLET | 10 mg | ORAL | ANDA | 19 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 29033-028 | TABLET | 5 mg | ORAL | ANDA | 14 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 29033-029 | TABLET | 10 mg | ORAL | ANDA | 14 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 57664-655 | TABLET | 5 mg | ORAL | ANDA | 21 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 57664-656 | TABLET | 10 mg | ORAL | ANDA | 21 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62559-560 | TABLET | 5 mg | ORAL | ANDA | 19 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62559-561 | TABLET | 10 mg | ORAL | ANDA | 19 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-4828 | TABLET | 5 mg | ORAL | ANDA | 21 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68151-1320 | TABLET | 5 mg | ORAL | ANDA | 21 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68151-3005 | TABLET | 10 mg | ORAL | ANDA | 21 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69367-421 | TABLET | 5 mg | ORAL | ANDA | 22 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69367-422 | TABLET | 10 mg | ORAL | ANDA | 22 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72162-2652 | TABLET | 5 mg | ORAL | ANDA | 21 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72162-2653 | TABLET | 10 mg | ORAL | ANDA | 21 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72789-099 | TABLET | 10 mg | ORAL | ANDA | 18 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72789-100 | TABLET | 5 mg | ORAL | ANDA | 18 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72789-293 | TABLET | 10 mg | ORAL | ANDA | 21 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72789-293 | TABLET | 10 mg | ORAL | ANDA | 21 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72789-294 | TABLET | 5 mg | ORAL | ANDA | 21 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72789-294 | TABLET | 5 mg | ORAL | ANDA | 21 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 76385-131 | TABLET | 5 mg | ORAL | ANDA | 18 sections |
| Pindolol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 76385-132 | TABLET | 10 mg | ORAL | ANDA | 18 sections |