tolazoline 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antihistaminics or local vasoconstrictors, antazoline derivatives | 2695 | 59-98-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A vasodilator that apparently has direct actions on blood vessels and also increases cardiac output. Tolazoline can interact to some degree with histamine, adrenergic, and cholinergic receptors, but the mechanisms of its therapeutic effects are not clear. It is used in treatment of persistent pulmonary hypertension of the newborn.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 75 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 12.48 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 17, 1948 | FDA | NOVARTIS |
FDA Adverse Event Reporting System (Female)
None
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 | C04AB02 | CARDIOVASCULAR SYSTEM PERIPHERAL VASODILATORS PERIPHERAL VASODILATORS Imidazoline derivatives |
| ATC | M02AX02 | MUSCULO-SKELETAL SYSTEM TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN Other topical products for joint and muscular pain |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D000317 | Adrenergic alpha-Antagonists |
| MeSH PA | D018674 | Adrenergic Antagonists |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D014665 | Vasodilator Agents |
| CHEBI has role | CHEBI:35620 | vasodilator agents |
| CHEBI has role | CHEBI:35674 | antihypertensive drugs |
| CHEBI has role | CHEBI:37890 | alpha-adrenergic receptor blockaders |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Disorder of blood vessel | indication | 27550009 | DOID:178 |
| Cerebrovascular disease | indication | 62914000 | DOID:6713 |
| Persistent pulmonary hypertension of the newborn | indication | 233815004 | DOID:13042 |
| Dysmenorrhea | off-label use | 266599000 | |
| Tachyarrhythmia | contraindication | 6285003 | |
| Low blood pressure | contraindication | 45007003 | |
| Arterial hemorrhage | contraindication | 234003006 |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Horses | To antagonize the effect of xylazine | Indication |
| Horses | Treatment of Patnaik grade II or III, recurrent, cutaneous mast cell tumors with or without regional lymph node involvement | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| Tolazine Injection | Akorn Animal Health Inc. | 1 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.97 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Alpha-2A adrenergic receptor | GPCR | ANTAGONIST | Ki | 6.64 | WOMBAT-PK | CHEMBL | |||
| Alpha-1A adrenergic receptor | GPCR | ANTAGONIST | Ki | 5.50 | WOMBAT-PK | CHEMBL | |||
| Alpha-2B adrenergic receptor | GPCR | ANTAGONIST | Ki | 5.50 | WOMBAT-PK | CHEMBL | |||
| Alpha-2C adrenergic receptor | GPCR | ANTAGONIST | Ki | 5.43 | WOMBAT-PK | CHEMBL | |||
| Trace amine-associated receptor 1 | GPCR | Ki | 5.79 | CHEMBL | |||||
| Adrenergic receptor alpha-2 | GPCR | Ki | 6.74 | CHEMBL | |||||
| Adrenergic receptor alpha-1 | GPCR | IC50 | 5.68 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019951 | VUID |
| N0000148036 | NUI |
| D00997 | KEGG_DRUG |
| 59-97-2 | SECONDARY_CAS_RN |
| 4018790 | VANDF |
| 4019951 | VANDF |
| C0040373 | UMLSCUI |
| CHEBI:28502 | CHEBI |
| CHEMBL770 | ChEMBL_ID |
| DB00797 | DRUGBANK_ID |
| CHEMBL1689 | ChEMBL_ID |
| D014043 | MESH_DESCRIPTOR_UI |
| 5504 | PUBCHEM_CID |
| 4213 | INN_ID |
| 7310 | IUPHAR_LIGAND_ID |
| CHH9H12AQ3 | UNII |
| 10634 | RXNORM |
| 5594 | MMSL |
| d00741 | MMSL |
| 001844 | NDDF |
| 004739 | NDDF |
| 19041007 | SNOMEDCT_US |
| 363554004 | SNOMEDCT_US |
| 4220008 | SNOMEDCT_US |
Pharmaceutical products:
None