aminosalicylic acid Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2050 | 65-49-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An antitubercular agent often administered in association with ISONIAZID. The sodium salt of the drug is better tolerated than the free acid.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 12 | g | O |
| 14 | g | O |
| 14 | g | P |
| 15 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 142.85 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 2 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 1306.01 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 8, 1950 | FDA | CONSOLIDATED MIDLAND |
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 |
|---|---|---|---|---|---|---|
| Drug resistance | 130.17 | 51.59 | 23 | 181 | 2601 | 2355280 |
| Electrocardiogram QT prolonged | 116.48 | 51.59 | 25 | 179 | 7789 | 2350092 |
| Anaemia | 83.67 | 51.59 | 26 | 178 | 34766 | 2323115 |
| Neuropathy peripheral | 75.84 | 51.59 | 19 | 185 | 11413 | 2346468 |
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 |
|---|---|---|---|---|---|---|
| Electrocardiogram QT prolonged | 250.25 | 61.74 | 50 | 206 | 5495 | 1741030 |
| Hepatotoxicity | 201.03 | 61.74 | 38 | 218 | 3046 | 1743479 |
| Tuberculosis | 114.67 | 61.74 | 22 | 234 | 1844 | 1744681 |
| Drug resistance | 96.95 | 61.74 | 21 | 235 | 3209 | 1743316 |
| Anaemia | 80.17 | 61.74 | 29 | 227 | 29428 | 1717097 |
| Intentional product use issue | 66.61 | 61.74 | 15 | 241 | 2704 | 1743821 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J04AA01 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIMYCOBACTERIALS DRUGS FOR TREATMENT OF TUBERCULOSIS Aminosalicylic acid and derivatives |
| ATC | J04AA02 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIMYCOBACTERIALS DRUGS FOR TREATMENT OF TUBERCULOSIS Aminosalicylic acid and derivatives |
| ATC | J04AA03 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIMYCOBACTERIALS DRUGS FOR TREATMENT OF TUBERCULOSIS Aminosalicylic acid and derivatives |
| CHEBI has role | CHEBI:33231 | antitubercular agent |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000995 | Antitubercular Agents |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Acute tuberculosis | indication | 25629007 | |
| Pulmonary tuberculosis | indication | 154283005 | DOID:2957 |
| Crohn's disease | off-label use | 34000006 | |
| Ulcerative colitis | off-label use | 64766004 | DOID:8577 |
| Goiter | contraindication | 3716002 | DOID:12176 |
| Peptic ulcer | contraindication | 13200003 | DOID:750 |
| Hypokalemia | contraindication | 43339004 | |
| Crystalluria | contraindication | 46784006 | |
| Chronic heart failure | contraindication | 48447003 | |
| Acidosis | contraindication | 51387008 | |
| Duodenal ulcer disease | contraindication | 51868009 | DOID:1724 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Anemia due to enzyme deficiency | contraindication | 111577008 | |
| Deficiency of glucose-6-phosphate dehydrogenase | contraindication | 124134002 | DOID:2862 |
| Cobalamin deficiency | contraindication | 190634004 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Gastric ulcer | contraindication | 397825006 | DOID:10808 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.71 | acidic |
| pKa2 | 12.94 | acidic |
| pKa3 | 2.33 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Cyclooxygenase | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
| Tyrosine-protein phosphatase non-receptor type 1 | Enzyme | Kd | 2.92 | CHEMBL | |||||
| 2-amino-4-hydroxy-6-hydroxymethyldihydropteridine pyrophosphokinase | Kinase | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4018852 | VUID |
| N0000180192 | NUI |
| C0030125 | UMLSCUI |
| D00162 | KEGG_DRUG |
| 5B2658E0N2 | UNII |
| 133-09-5 | SECONDARY_CAS_RN |
| 255666002 | SNOMEDCT_US |
| 417238004 | SNOMEDCT_US |
| 10002 | MMSL |
| 4176 | MMSL |
| d04226 | MMSL |
| 4018852 | VANDF |
| 7833 | RXNORM |
| 002845 | NDDF |
| 4649 | PUBCHEM_CID |
| CHEBI:27565 | CHEBI |
| CHEMBL1169 | ChEMBL_ID |
| DB00233 | DRUGBANK_ID |
| CHEMBL1200584 | ChEMBL_ID |
| CHEMBL1200966 | ChEMBL_ID |
| D010131 | MESH_DESCRIPTOR_UI |
| CHEMBL2096646 | ChEMBL_ID |
| CHEMBL2105983 | ChEMBL_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Paser | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49938-107 | GRANULE, DELAYED RELEASE | 4 g | ORAL | ANDA | 12 sections |