nalidixic acid 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antibacterials, nalidixic acid derivatives | 1875 | 389-08-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A synthetic 1,8-naphthyridine antimicrobial agent with a limited bacteriocidal spectrum. It is an inhibitor of the A subunit of bacterial DNA GYRASE.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 4 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.43 mg/mL | Bocci G, Oprea TI, Benet LZ |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 287.20 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 96 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 6, 1964 | 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 |
|---|---|---|---|---|---|---|
| Idiopathic intracranial hypertension | 25.79 | 23.51 | 3 | 3 | 2928 | 63486088 |
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 | J01MB02 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE QUINOLONE ANTIBACTERIALS Other quinolones |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D059005 | Topoisomerase II Inhibitors |
| MeSH PA | D059003 | Topoisomerase Inhibitors |
| CHEBI has role | CHEBI:33281 | antibiotics |
| CHEBI has role | CHEBI:36047 | antibacterial drugs |
| CHEBI has role | CHEBI:59517 | DNA synthesis inhibitors |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Bacterial urinary infection | indication | 312124009 | |
| Disorder of the central nervous system | contraindication | 23853001 | DOID:331 |
| Tendinitis | contraindication | 34840004 | DOID:971 |
| Acute nephropathy | contraindication | 58574008 | |
| Anemia due to enzyme deficiency | contraindication | 111577008 | |
| Deficiency of glucose-6-phosphate dehydrogenase | contraindication | 124134002 | DOID:2862 |
| Seizure disorder | contraindication | 128613002 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Peripheral nerve disease | contraindication | 302226006 | |
| Pseudomembranous enterocolitis | contraindication | 397683000 | |
| Traumatic rupture of tendon | contraindication | 415749005 | |
| Porphyria | contraindication | 418470004 | |
| Severe Cerebral Arteriosclerosis | contraindication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 6.27 | acidic |
| pKa2 | 0.86 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 2B | GPCR | IC50 | 5.10 | WOMBAT-PK | |||||
| Pyruvate kinase PKM | Enzyme | IC50 | 4.28 | CHEMBL | |||||
| DNA gyrase | Enzyme | INHIBITOR | CHEMBL | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4018247 | VUID |
| N0000146578 | NUI |
| D00183 | KEGG_DRUG |
| 4018247 | VANDF |
| C0027353 | UMLSCUI |
| CHEBI:100147 | CHEBI |
| NIX | PDB_CHEM_ID |
| CHEMBL5 | ChEMBL_ID |
| DB00779 | DRUGBANK_ID |
| D009268 | MESH_DESCRIPTOR_UI |
| 4421 | PUBCHEM_CID |
| 12773 | IUPHAR_LIGAND_ID |
| 1450 | INN_ID |
| 3B91HWA56M | UNII |
| 618425 | RXNORM |
| 2063 | MMSL |
| 5148 | MMSL |
| d00157 | MMSL |
| 002860 | NDDF |
| 387261006 | SNOMEDCT_US |
| 47602007 | SNOMEDCT_US |
Pharmaceutical products:
None