Dosing and uses of Paser (aminosalicylic acid)
Adult dosage forms and strengths
oral granules, delayed-release
- 4g/packet
Tuberculosis
Indicated for treatment of TB in combination with other active agents; most commonly used in regimens for multi-drug resistant TB or when intolerance to other antitubercular agents occurs
4 g PO TId
Mix granules in acidic liquid or sprinkle on acidic food (see Administration)
Ulcerative Colitis (Orphan)
Treatment of mild-to-moderate ulcerative colitis in patients intolerant to sulfasalazine
Orphan indication sponsor
- Beeken, Warren M.D.; University Of Vermont, Given C-317; Burlington, VT 05405
Renal & Hepatic Impairment
Hepatic impairment: Caution advised
Renal impairment
- CrCl 10-50 mL/min: Decrease dose by 25-50%
- CrCl <10 mL/min: Decrease dose by 50%
- Hemodialysis: Administer 50% of dose after dialysis
Administration
Mix granules in acidic liquid or sprinkle on food (ie, pH <5) such as, apple sauce, yogurt, tomato or orange juice
Granules are protected by an enteric coating absorption does not commence until they leave the stomach; the soft skeletons of the granules remain and may be seen in the stooL
Patients who have neutralized gastric acid with antacids will not need to protect the acid resistant coating with an acidic food since no acid is present to spoil the drug
Store granules before use in refrigerator or freezer (ie, below 59°F [15°C]); may store at room temperature for show periods of time
Avoid excessive heat; do not use if packet becomes swollen or granules have lost tan color and have turned dark brown or purple
Pediatric dosage forms and strengths
oral granules, delayed-release
- 4g/packet
Tuberculosis
Indicated for treatment of TB in combination with other active agents; most commonly used in regimens for multi-drug resistant TB or when intolerance to other antitubercular agents occurs
200-300 mg/kg/day PO divided in 2-4 equal doses; not to exceed 10 g/day
Mix granules in acidic liquid or sprinkle on acidic food (see Administration)
Crohn Disease (Orphan)
Treatment of acute flares in pediatric patients with ileocecal Crohn disease
Orphan indication sponsor
- Jacobus Pharmaceutical Co., Inc. 37 Cleveland Lane Princeton, NJ 08540
Renal & Hepatic Impairment
Hepatic impairment: Caution advised
Renal impairment
- CrCl 10-50 mL/min: Decrease dose by 25-50%
- CrCl <10 mL/min: Decrease dose by 50%
- Hemodialysis: Administer 50% of dose after dialysis
Administration
Mix granules in acidic liquid or sprinkle on food (ie, pH <5) such as, apple sauce, yogurt, tomato or orange juice
Granules are protected by an enteric coating absorption does not commence until they leave the stomach; the soft skeletons of the granules remain and may be seen in the stooL
Patients who have neutralized gastric acid with antacids will not need to protect the acid resistant coating with an acidic food since no acid is present to spoil the drug
Store granules before use in refrigerator or freezer (ie, below 59°F [15°C]); may store at room temperature for show periods of time
Avoid excessive heat; do not use if packet becomes swollen or granules have lost tan color and have turned dark brown or purple
Paser (aminosalicylic acid) adverse (side) effects
Frequency not defined
GI intolerance manifested by nausea, vomiting, diarrhea, and abdominal pain
Hypersensitivity reactions: Fever, skin eruptions of various types, including exfoliative dermatitis, infectious mononucleosis-like, or lymphoma-like syndrome, leucopenia, agranulocytosis, thrombocytopenia, Coombs' positive hemolytic anemia, jaundice, hepatitis, pericarditis, hypoglycemia, optic neuritis, encephalopathy, Leoffler's syndrome, vasculitis and a reduction in prothrombin
Crystalluria (prevent by maintaining urine at neutral or alkaline pH)
Warnings
Contraindications
Hypersensitivity
End-stage renal disease
Cautions
Monitor liver function; reports of drug-induced hepatitis with rapidly absorbed aminosalicylic acid preparations
Pregnancy and lactation
Pregnancy category: C
Lactation: Distributed in human breast milk; caution advised
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Paser (aminosalicylic acid)
Mechanism of action
Bacteriostatic against Mycobacterium tuberculosis; inhibits onset of bacterial resistance to streptomycin and isoniazid
Mechanism of action postulated to be inhibition of folic acid synthesis (but without potentiation with antifolic compounds) and/or inhibition of synthesis of the cell wall component, mycobactin, thus reducing iron uptake by M. tuberculosis
Absorption
Peak Plasma Time: Initial time 2 hr (range 45 min to 24 hr); median time 6 hr (range 1.5-24 hr
Peak Plasma Concentration: Initial 2 mcg/mL (ASA); mean 20 mcg/mL
Distribution
Protein Bound: 50-60%
Penetration into CSF with inflamed meninges
Metabolism
Metabolized by acetylation
After 2 hr in simulated gastric fluid, 10% of unprotected aminosalicylic acid is decarboxylated to form meta-aminophenol, a known hepatotoxin
Elimination
Excretion: Urine 80%, with 50% in acetylated form
