Aminosalicylic Acid
Pronunciation
(a mee noe sal i SIL ik AS id)
U.S. Brand Names
Paser®
Synonyms
Aminosalicylate Sodium; 4-Aminosalicylic Acid; Para-Aminosalicylate Sodium; PAS; Sodium PAS
Generic Available
No
Canadian Brand Names
Nemasol® Sodium
Use
Adjunctive treatment of tuberculosis used in combination with other antitubercular agents
Use - Unlabeled/Investigational
Crohn's disease
Pregnancy Risk Factor
C
Pregnancy Implications
Teratogenic effects have been reported in animals, however, adequate studies have not been done in humans. Use during pregnancy only if clearly needed.
Lactation
Enters breast milk/not recommended
Contraindications
Hypersensitivity to aminosalicylic acid or any component of the formulation
Warnings/Precautions
Use with caution in patients with hepatic or renal dysfunction and patients with gastric ulcer.
Adverse Reactions
Frequency not defined.
Cardiovascular: Pericarditis, vasculitis
Central nervous system: Encephalopathy, fever
Dermatologic: Skin eruptions
Endocrine & metabolic: Goiter (with or without myxedema), hypoglycemia
Gastrointestinal: Abdominal pain, diarrhea, nausea, vomiting
Hematologic: Agranulocytosis, anemia (hemolytic), leukopenia, thrombocytopenia
Hepatic: Hepatitis, jaundice
Ocular: Optic neuritis
Respiratory: Eosinophilic pneumonia
Overdosage/Toxicology
Acute overdose results in crystalluria and renal failure, nausea, and vomiting. Alkalinization of urine with sodium bicarbonate and forced diuresis can prevent crystalluria and nephrotoxicity.
Drug Interactions
Digoxin: Serum levels may be decreased by aminosalicylic acid.
Vitamin B12: Serum levels may be decreased by aminosalicylic acid.
Stability
Prior to dispensing, store granules below 15°C (59°F). Once dispensed, packets may be stored at room temperature for short periods of time. Do not use if packet is swollen or if granules are dark brown or purple.
Mechanism of Action
Aminosalicylic acid (PAS) is a highly specific bacteriostatic agent active against
M. tuberculosis
. Structurally related to para-aminobenzoic acid (PABA) and its mechanism of action is thought to be similar to the sulfonamides, a competitive antagonism with PABA; disrupts plate biosynthesis in sensitive organisms.
Pharmacodynamics/Kinetics
Absorption: Readily, >90%
Protein binding: 50% to 60%
Metabolism: Hepatic (>50%) via acetylation
Half-life elimination: Reduced with renal impairment
Time to peak, serum: 6 hours
Excretion: Urine (>80% as unchanged drug and metabolites)
Dosage
Oral:
Children: Tuberculosis: 200-300 mg/kg/day in 3-4 equally divided doses
Adults:
Tuberculosis: 150 mg/kg/day in 2-3 equally divided doses
Crohn's disease (unlabeled use): 1.5 g/day
Dosing adjustment in renal impairment:
Clcr 10-50 mL/minute: Administer 50% to 75% of dose
Clcr<10 mL/minute: Administer 50% of dose
Administer after hemodialysis: Administer 50% of dose
Continuous arteriovenous hemofiltration: Dose for Clcr<10 mL/minute
Administration
Do not use granules if packet is swollen or if granules are discolored (ie, brown or purple). Granules may be sprinkled on applesauce or yogurt (do not chew) or suspended in tomato or orange juice.
Dietary Considerations
May be taken with food.
Patient Education
May be taken with food; may sprinkle on applesauce or yogurt, or suspend in tomato or orange juice. Do not use granules if discolored (brown or purple) or if packet is swollen; see pharmacist for new prescription. Do not stop taking without consulting prescriber. Report persistent sore throat, fever, unusual bleeding or bruising, persistent nausea or vomiting, or abdominal pain.
Pregnancy/breast-feeding precautions:
Inform prescriber if you are or intend to become pregnant. Breast-feeding is not recommended.
Dental Health: Effects on Dental Treatment
NSAID formulations are known to reversibly decrease platelet aggregation via mechanisms different than observed with aspirin. The dentist should be aware of the potential of abnormal coagulation. Caution should also be exercised in the use of NSAIDs in patients already on anticoagulant therapy with drugs such as warfarin (Coumadin®).
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
None reported
Mental Health: Effects on Psychiatric Treatment
May cause bone marrow suppression; use caution with clozapine and carbamazepine
Dosage Forms
Granules: 4 g/packet (30s) [contains talc]
References
Davidson PT and Le HQ, "Drug Treatment of Tuberculosis - 1992,"
Drugs
, 1992, 43(5):651-73.
"Drugs for Tuberculosis,"
Med Lett Drugs Ther
, 1993, 35(908):99-101.
Iseman MD, "Treatment of Multidrug-Resistant Tuberculosis,"
N Engl J Med
, 1993, 329(11):784-91.
International Brand Names
Mesacol® (BD, IN, TH); Nemasol® Sodium (CA); Pasalba® (AU); Pas Atlantic® (TH); Pas-Fatol N® (DE); PAS® (TR); Quadrasa® (FR, IT)
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