4-aminosalicylate
4-aminosalicylate Uses, Dosage, Side Effects, Food Interaction and all others data.
An antitubercular agent often administered in association with isoniazid. The sodium salt of the drug is better tolerated than the free acid.
4-aminosalicylate is an anti-mycobacterial agent used with other anti-tuberculosis drugs (most often isoniazid) for the treatment of all forms of active tuberculosis due to susceptible strains of tubercle bacilli. The two major considerations in the clinical pharmacology of aminosalicylic acid are the prompt production of a toxic inactive metabolite under acid conditions and the short serum half life of one hour for the free drug. 4-aminosalicylate is bacteriostatic against Mycobacterium tuberculosis (prevents the multiplying of bacteria without destroying them). It also inhibits the onset of bacterial resistance to streptomycin and isoniazid.
| Trade Name | 4-aminosalicylate |
| Generic | Aminosalicylic acid |
| Aminosalicylic acid Other Names | 4-aminosalicylate, 4-aminosalicylic acid, Aminosalicylic acid, p-aminosalicylic acid, para-amino salicylic acid, para-aminosalicylic acid |
| Type | |
| Formula | C7H7NO3 |
| Weight | Average: 153.1354 Monoisotopic: 153.042593095 |
| Protein binding | 50-60% |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
4-aminosalicylate is an aminosalicylate drug used to induce remission in ulcerative colitis.
For the treatment of tuberculosis
4-aminosalicylate is also used to associated treatment for these conditions: Tuberculosis (TB)
How 4-aminosalicylate works
There are two mechanisms responsible for aminosalicylic acid's bacteriostatic action against Mycobacterium tuberculosis. Firstly, aminosalicylic acid inhibits folic acid synthesis (without potentiation with antifolic compounds). The binding of para-aminobenzoic acid to pteridine synthetase acts as the first step in folic acid synthesis. 4-aminosalicylate binds pteridine synthetase with greater affinity than para-aminobenzoic acid, effectively inhibiting the synthesis of folic acid. As bacteria are unable to use external sources of folic acid, cell growth and multiplication slows. Secondly, aminosalicylic acid may inhibit the synthesis of the cell wall component, mycobactin, thus reducing iron uptake by M. tuberculosis.
Toxicity
LD50=4 gm/kg (orally in mice); LD50=3650 mg/kg (orally in rabbits)
Food Interaction
- Take with or without food. The absorption is unaffected by food.
Innovators Monograph
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