      Document 0047
 DOCN  DRG0047
 UNIQUE IDENTIFIER        DRG-0200
 NAME OF SUBSTANCE        Aminosalicylic acid [USAN 1996]
 REGISTRY NUMBER          65-49-6
 STANDARD CHEMICAL NAME   4-Amino-2-hydroxybenzoic acid [Merck Index
                          1989]
 SYNONYMS                 Paser Granules [PDR 1995]
 SYNONYMS                 PAS [Merck Index 1989]
 SYNONYMS                 4-Aminosalicylic acid [Merck Index 1989]
 SYNONYMS                 p-Aminosalicylic acid [Merck Index 1989]
 SYNONYMS                 Deapasil [Merck Index 1989]
 SYNONYMS                 Apas [Merck Index 1989]
 SYNONYMS                 Apacil [Merck Index 1989]
 SYNONYMS                 Hellipidyl [Merck Index 1989]
 SYNONYMS                 PAS-C [Merck Index 1989]
 SYNONYMS                 Pamacyl [Merck Index 1989]
 SYNONYMS                 Parasal [Merck Index 1989]
 SYNONYMS                 Pascorbic [Merck Index 1989]
 SYNONYMS                 Pasolac [Merck Index 1989]
 SYNONYMS                 Parasalicil [Merck Index 1989]
 SYNONYMS                 Parasalindon [Merck Index 1989]
 SYNONYMS                 Pasnodia [Merck Index 1989]
 SYNONYMS                 Propasa [Merck Index 1989]
 SYNONYMS                 Rezipas [Merck Index 1989]
 SYNONYMS                 Sanipirol-4 [Merck Index 1989]
 SYNONYMS                 Pamisyl [Merck Index 1989]
 SYNONYMS                 Para-Pas [Merck Index 1989]
 SYNONYMS                 para-Aminosalicylic acid [CHEMLINE]
 PROTOCOL ID NUMBERS      NIAID ACTG 238
 SECONDARY SOURCE ID      NSC-2083 [CHEMLINE]
 SECONDARY SOURCE ID      HSDB 3203 [CHEMLINE]
 PHARMACOLOGICAL ACTION   MODE OF ACTION: Bacteriostatic in action.
                          Mechanism of action is similar to that of
                          sulfonamides. Prevents the synthesis of folic
                          acid in susceptible organisms by
                          competitively blocking the conversion of
                          aminobenzoic acid to dihydrofolic acid. The
                          activity of aminosalicylic acid is partially
                          blocked by aminobenzoic acid. Active only
                          against M. tuberculosis. Resistant strains of
                          initially susceptible organisms develop
                          rapidly if aminosalicylic acid is used alone
                          in treatment of clinical tuberculosis. This
                          can be delayed or prevented by concurrent
                          treatment with other antituberculosis drugs.
                          Inhibits the onset of resistance to
                          streptomycin and isoniazid. Is readily
                          absorbed from the intestinal tract. Acid
                          resistant coatings of the drug (e.g., Paser
                          granules) protect against degradation in the
                          stomach to meta-aminophenol, a known
                          hepatotoxin. Excretion is through the kidneys
                          (80%) with 50% or more of the dosage being
                          excreted in the acetylated form. [PDR 1995]
                          [AHFS Drug Information 1995]
 DISEASES STUDIED/TREATED Treatment of multi-drug resistant pulmonary
                          tuberculosis [NIAID ACTG 238]
 CLASSIFICATION CODE      Antibacterial [USAN 1996]
 ADVERSE EFFECTS          Adverse effects include gastrointestinal
                          disturbances, rash, fever, fatal drug-induced
                          hepatitis, malabsorption syndrome,
                          leukopenia, granulocytosis, Coombs positive
                          hemolytic anemia, pericarditis, optic
                          neuritis. [PDR 1995]
 CONTRAINDICATIONS        Contraindicated in impaired renal or hepatic
                          functions and in patients with gastric
                          ulcers. [AHFS Drug Information 1995]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: The 4-amino derivative of a
                          group of hydroxybenzoic acids. Bacteriostatic
                          agent [MeSH; NIAID ACTG 238]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C7H7NO3 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 153.14 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MELTING POINT: 150-151 C [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   ELEMENTAL COMP: C54.90%, H4.61%, N9.15%,
                          O31.34% [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   SOLUBILITY: Soluble in water, alcohol, dilute
                          nitric acid, dilute sodium hydroxide.
                          Slightly soluble in ether. Practically
                          insoluble in benzene [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   STABILITY: Unstable in a moist environment
                          and will discolor [NIAID ACTG 238]
 CHEMICAL/PHYSICAL DATA   PHYSICAL COMMENT: pKa: 3.25 [Merck Index
                          1989]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: 4 g packets. [AHFS Drug
                          Information 1995]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Oral. [AHFS Drug
                          Information 1995]
 SUBSTANCE DELIVERY DATA  STORAGE: Store below 77 F (25 C). [PDR 1995]
 MANUFACTURERS            Jacobus Pharmaceutical Company
 REFERENCES               Peloquin CA, Henshaw TL, Huitt GA, Berning
                          SE, Nitta AT, James GT. Pharmacokinetic
                          evaluation of para-aminosalicylic acid
                          granules. Pharmacotherapy. 1994
                          Jan-Feb;1491):40-6.
 REFERENCES               Heifets LB. Antimycobacterial drugs. Semin
                          Respir Infect. 1994 Jun;9(2):84-103.
 REFERENCES               Peloquin CA. Pharmacology of the
                          antimycobacterial drugs. Med Clin North Am.
                          1993 Nov;77(6):1253-62.
 REFERENCES               Shah A, Bhagat R, Panchal N. Resistant
                          tuberculosis: successful treatmemt with
                          amikacin, ofloxacin, clofazimine, and pas
                          [letter]. Tuber Lung Dis. 1993
                          Feb;74(1):64-5.
 REFERENCES               el-Chaar GM, Schwenk MH, Bardini J, Caliendo
                          G, Frank  C, Profeta LM, Talbot KA, Cohen H.
                          New drugs on the horizon. Clin Podiatr Med
                          Surg. 1992 Apr;9(2):481-501.
 ENTRY MONTH              9403
 LAST REVISION DATE       951024
 

SOURCE: National Library of Medicine, Bethesda, MD.  Distributed by AEGIS.
