Aminosalicylic Acid
Name: Aminosalicylic Acid
- Aminosalicylic Acid drug
- Aminosalicylic Acid dosage
- Aminosalicylic Acid names
- Aminosalicylic Acid adverse effects
- Aminosalicylic Acid side effects
Description
PASER (aminosalicylic acid) granules are a delayed release granule preparation of aminosalicylic acid (p-aminosalicylic acid: 4-aminosalicylic acid) for use with other anti-tuberculosis drugs for the treatment of all forms of active tuberculosis due to susceptible strains of tubercle bacilli. The granules are designed for gradual release to avoid high peak levels not useful (and perhaps toxic) with bacteriostatic drugs. Aminosalicylic acid is rapidly degraded in acid media; the protective acid-resistant outer coating is rapidly dissolved in neutral media so a mildly acidic food such as orange, apple or tomato juice, yogurt or apple sauce should be used.
Aminosalicylic acid (p-aminosalicylic acid) is 4-Amino-2-hydroxybenzoic acid. PASER granules are the free base of aminosalicylic acid and do NOT contain sodium or a sugar. The molecular formula is C 7 H 7 NO 3 with a molecular weight of 153.14. With heat p-aminosalicylic acid is decarboxylated to produce CO 2 and m-aminophenol. If the airtight packets are swollen, storage has been improper. DO NOT USE if packets are swollen or the granules have lost their tan color and are dark brown or purple.
The structural formula is:
PASAR granules are supplied as off-white tan colored granules with an average diameter of 1.5 mm and an average content of 60% aminosalicylic acid by weight. The acid resistant outer coating will be completely removed by a few minutes at a neutral pH. The inert ingredients are:
colloidal silicon dioxide
dibutyl sebacate
hydroxypropyl methyl cellulose
methacrylic acid copolymer
microcystalline cellulose
talc
The packets contain 4 grams of aminosalicylic acid for oral administration three times a day by sprinkling an apple sauce or yogurt to be eaten without chewing. Suspension in an acidic fruit drink such as orange juice or tomato juice will protect the coating for at least 2 hours. Swirling the juice in the glass will help resuspend the granules if they sink.
Overdose
Overdosage has not been reported.
Patient information
The patient should be advised that the first signs of hypersensitivity include a rash, often followed by fever, and much less frequently, GI disturbances of anorexia, nausea or diarrhea. If such symptoms develop, the patient should immediately cease taking the medication and arrange for a prompt clinical visit.
Patients should be advised that poor compliance in taking anti-TB medication often leads to treatment failure, and, not infrequently, to the development of resistance of the organisms in the individual patient.
Patients should be advised that the skeleton of the granules may be seen in the stool.
The coating to protect the PASER (aminosalicylic acid) granules dissolves promptly under neutral conditions; the granules therefore should be administered by sprinkling on acidic foods such as apple sauce or yogurt or by suspension in a fruit drink which will protect the coating, but the granules sink and will have to be swirled. The coating will last at least 2 hours in either system. All juices tested to date have been satisfactory; tested are: tomato, orange, grapefruit, grape, cranberry, apple, "fruit punch".
Patients should be advised to store PASER (aminosalicylic acid) in a refrigerator or freezer. PASER (aminosalicylic acid) packets may be stored at room temperature for short periods of time.
Patients should be advised NOT to use if the packets are swollen or the granules have lost their tan color and are dark brown or purple. The patient should inform the pharmacist or physician immediately and return the medication.
Interactions for Aminosalicylic Acid
Specific Drugs
| Drug | Interaction | Comments |
|---|---|---|
| Ammonium chloride | Increased risk of crystalluriaa | Do not use concomitantlya |
| Anticoagulants, oral | Enhanced hypoprothrombinemic effecta | Anticoagulant dosage adjustment may be necessarya |
| Diphenhydramine | Impaired GI absorption of aminosalicylic acida | Avoid concurrent usea |
| Digoxin | Decreased GI absorption of digoxin100 101 102 | |
| Isoniazid | Reduced rate of acetylation of isoniazid (especially in rapid acetylators) reported with some aminosalicylic acid preparations; appears to be dose related102 Interaction not studied using commercially available aminosalicylic acid delayed-release granules (Paser);102 a the lower serum concentrations produced by the delayed-release preparation should result in a reduced effect on acetylation of isoniazid102 | Not considered clinically importanta |
| Probenecid | Conflicting reports, but does not appear to increase plasma concentrations of aminosalicylic acid 102 | |
| Rifampin | Decreased serum rifampin concentrations reported with certain aminosalicylic acid preparations;102 a not reported with commercially available aminosalicylic acid delayed-release granules (Paser)102 a | May be caused by an excipient not included in commercially available aminosalicylic acid delayed-release granules (Paser)102 |
| Vitamin B12 | Decreased oral absorption of vitamin B12; clinically important erythrocyte abnormalities reported102 | Consider use of maintenance vitamin B12 treatment in those receiving aminosalicylic acid for >1 month102 |
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
| Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
| Oral | Granules, delayed-release (enteric-coated) | 4 g/packet | Paser | Jacobus |
Index Terms
- 4-Aminosalicylic Acid
- Aminosalicylate Calcium
- Aminosalicylate Sodium
- Para-Aminosalicylate Sodium
- Para-Aminosalicylic Acid
- PAS
- Sodium PAS
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Packet, Oral:
Paser: 4 g (30 ea)
Special Populations Renal Function Impairment
Drug and its acetyl metabolite may accumulate.
Dosing Geriatric
Refer to adult dosing.
Warnings/Precautions
Concerns related to adverse effects:
• Salicylate sensitivity: Patients with sensitivity to tartrazine dyes, nasal polyps, and asthma may have an increased risk of salicylate sensitivity.
Disease-related concerns:
• Gastric ulcer: Use with caution in patients with gastric ulcer.
• Hepatic impairment: Use with caution in patients with hepatic impairment.
• Renal impairment: Use with caution in patients with renal impairment; contraindicated in patients with severe renal impairment.
In Summary
More frequently reported side effects include: eosinophilia and leukocytosis. See below for a comprehensive list of adverse effects.