Liver Function
In one retrospective study of 7492 patients on rapidly absorbed aminosalicylic acid preparations, drug-induced hepatitis occurred in 38 patients (0.5%); in these 38 the first symptom usually appeared within three months of the start of therapy with a rash as the most common event followed by fever and much less frequently by GI disturbances of anorexia, nausea or diarrhea. Only one patient was diagnosed on routine biochemistry.
Premonitory symptoms in 90% of these 38 patients preceded jaundice by a few days to several weeks with the mean time of onset 33 days with a range of 7-90 days. Half of the adverse reactions occurred during the third, fourth or fifth weeks. When aminosalicylic acid-induced hepatitis was diagnosed, hepatomegaly was invariably present with lymphadenopathy in 46%, leucocytosis in 79%, and eosinophilia in 55%. Prompt recognition with discontinuation led to the recovery of all 38 patients. If recognized in the premonitory stage, the reaction is reported to “settle” in 24 hours and no jaundice ensues. From other reported studies failure to recognize the reaction can result in a mortality of up to 21%. The patient must be monitored carefully during the first three months of therapy and treatment must be discontinued immediately at the first sign of a rash, fever or other premonitory signs of intolerance.
There is currently no manufacturer warning information available for this drug.
PASER is indicated for the treatment of tuberculosis in combination with other active agents. It is most commonly used in patients with Multi-drug Resistant TB (MDR-TB) or in situations when therapy with isoniazid and rifampin is not possible due to a combination of resistance and/or intolerance. When PASER is added to the treatment regimen in patients proven or suspected drug resistance, it should be accompanied by at least one and preferably two other new agents to which the patient’s organism is known or expected to be susceptible.
PASER 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 C7H7NO3 with a molecular weight of 153.14. With heat p-aminosalicylic acid is decarboxylated to produce CO2 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:
PASER 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:
The packets contain 4 grams of aminosalicylic acid for oral administration three times a day by sprinkling on 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.