nail clipping [5.:<15 years of age or weighing 40 kg: 200 300 mg/kg daily (up to 10 g daily) given in 2 4 divided doses recommended by ATS, CDC, IDSA, and AAP. 104 107 Adolescents 15 years of age: 8 12 g daily given in 2 or 3 divided doses recommended by ATS, CDC, and IDSA. 104 Adults Tuberculosis Treatment of Active (Clinical) Tuberculosis Oral Manufacturer recommends 4 g 3 times daily. 102 8 12 g daily given in 2 or 3 doses recommended by ATS, CDC, and IDSA. 104 There is some evidence that 4 g twice daily achieves target serum concentrations. 104 109 Prescribing Limits Pediatric Patients Treatment of Active (Clinical) Tuberculosis Oral Maximum 10 g daily recommended by ATS, CDC, IDSA, and AAP. 104 107 Special Populations Hepatic Impairment Dosage adjustment not necessary, but increased clinical and laboratory monitoring recommended. 104 Clearance is not altered in patients with hepatic impairment, but these patients may not tolerate the drug as well as those with normal hepatic function. 102 Renal Impairment Contraindicated in severe renal disease (end-stage renal disease). 102 Some experts recommend 4 g twice daily for treatment of active TB in patients with Cl cr> <30 mL/minute or undergoing hemodialysis. 104 112 Doses should be given after hemodialysis 104 since the drug is removed by this procedure; 104 112 supplemental doses not necessary. 112 Cautions for Aminosalicylic Acid Contraindications Hypersensitivity to aminosalicylic acid or any ingredient in the formulation. 102 Severe renal disease (end-stage renal disease). 102 Warnings/Precautions Warnings Hepatic Effects Drug-induced hepatitis reported. 102 Prompt recognition of symptoms and discontinuance of aminosalicylic acid usually results in recovery; failure to recognize the reaction has resulted in fatalities. 102 Initial symptoms usually appear within 3 months after the drug is initiated. 102 Rash is the most common symptom; fever and GI disturbances (anorexia, nausea, diarrhea) may occur. 102 Premonitory symptoms usually precede jaundice by several days or weeks (mean time to onset is 33 days; range 7 90 days). 102 Hepatomegaly with lymphadenopathy, leukocytosis, and eosinophilia usually is present when hepatitis is diagnosed. 102 Monitor closely during the first 3 months of treatment. 102 Immediately discontinue the drug at the first sign of a rash, fever, or other premonitory signs of intolerance. 102 Sensitivity Reactions Hypersensitivity Reactions Hypersensitivity reactions, including fever, 102 skin eruptions of various types, 102 pruritus, a vasculitis, 102 exfoliative dermatitis, 102 joint pain, a eosinophilia, a leukopenia, 102 agranulocytosis, 102 thrombocytopenia, 102 hepatitis, 102 and jaundice, 102 reported. If manifestations of hypersensitivity occur (e.g., rash, fever), immediately discontinue all drugs. 102 After symptoms abate, cautiously reinitiate the drugs one at a time in small and gradually increasing doses to determine whether manifestations were drug-induced and, if so, which drug was responsible. 102 Desensitization Desensitization has been used when reinitiation of the drug was considered necessary in a patient who had a hypersensitivity reaction. 102 110 One desensitization procedure used successfully in 15 of 17 patients involved an initial 10-mg dose of the drug, doubling dosage every 2 days until a total daily dosage of 1 g was reached, then continuing dosage escalation while giving the total daily dosage in divided doses according to the usual administration schedule (i.e., 3 times daily). 102 If mild temperature elevation or skin reaction develops during the desensitization procedure, manufacturer states desensitization may be continued by decreasing the dosage by one increment (i.e., to the previous level at which no reaction occurred) or maintaining current dosage for another 2-day cycle before continuing dosage progression. 102 Such reactions are rare after a total daily aminosalicylic acid dosage of 1.5 g is reached. 102 General Precautions Precautions Related to Treatment of Tuberculosis Should not be used alone for treatment of active (clinical) TB; must be given in conjunction with other antituberculosis agents. 102 104 Clinical specimens for microscopic examination and mycobacterial cultures and in vitro susceptibility testing should be obtained prior to initiation of antituberculosis therapy and periodically during treatment to monitor therapeutic response. 104 The antituberculosis regimen should be modified as needed. 104 Patients with positive cultures after 4 months of treatment should be considered to have failed treatment (usually as the result of noncompliance or drug-resistant TB). 104 If added as a new drug to a regimen in patients experiencing treatment failure who have proven or suspected drug-resistant TB, at least 2 (preferably 3) new drugs known or expected to be active against the resistant strain should be added at the same time. 104 Compliance with the full course of antituberculosis therapy and all drugs included in the multiple-drug regimen is critical. 104 Missed doses increase the risk of treatment failure and increase the risk that M. tuberculosis will develop resistance to the antituberculosis regimen. 104 To ensure compliance, ATS, CDC, IDSA, and AAP recommend that directly observed (supervised) therapy (DOT) be used for treatment of active TB whenever possible, especially when intermittent regimens are used, when the patient is immunocompromised or infected with HIV, or when drug-resistant M. tuberculosis is involved. 104 107 Malabsorption Malabsorption of vitamin B 12 , folic acid, iron, and lipids has occurred, possibly as the result of increased peristalsis. a As a result of competition, a 5-g dose of aminosalicylic acid may reduce absorption of vitamin B 12 by about 55%; clinically important erythrocyte abnormalities may develop. 102 Consider using vitamin B 12 maintenance therapy in patients receiving aminosalicylic acid for> 1 month. 102 Laboratory Monitoring Assess hepatic enzyme concentrations and thyroid function prior to initiation of therapy. 104 Assess thyroid function every 3 months. 104 Specific Populations Pregnancy Category C. 102 ATS, CDC, and IDSA state that, although aminosalicylic acid has been used safely during pregnancy, the drug should be used in pregnant women only when there are no alternatives for treatment of MDR TB. 104 Lactation Distributed into milk. 102 Hepatic Impairment Use with caution. 102 Metabolism of aminosalicylic acid in patients with hepatic disease is comparable to that in healthy individuals, but such patients may tolerate aminosalicylic acid less well. 102 (See Hepatic Effects under Cautions.) Renal Impairment Use with caution. 102 Contraindicated in patients with severe renal disease (end-stage renal disease). 102 Patients with severe renal disease accumulate aminosalicylic acid and its acetyl metabolite but continue to acetylate the drug, resulting exclusively in the inactive acetylated form. 102 Common Adverse Effects GI effects (nausea, vomiting, abdominal pain, diarrhea). 102 Interactions for Aminosalicylic Acid Specific Drugs Drug Interaction Comments Ammonium chloride Increased risk of crystalluria a Do not use concomitantly a Anticoagulants, oral Enhanced hypoprothrombinemic effect a Anticoagulant dosage adjustment may be necessary a Diphenhydramine Impaired GI absorption of aminosalicylic acid a Avoid concurrent use a Digoxin Decreased GI absorption of digoxin 100 101 102 Isoniazid Reduced rate of acetylation of isoniazid (especially in rapid acetylators) reported with some aminosalicylic acid preparations; appears to be dose related 102 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 isoniazid 102 Not considered clinically important a 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 B 12 Decreased oral absorption of vitamin B 12 ; clinically important erythrocyte abnormalities reported 102 Consider use of maintenance vitamin B 12 treatment in those receiving aminosalicylic acid for >1 month 102 Aminosalicylic Acid Pharmacokinetics Absorption Bioavailability Readily absorbed from GI tract. a Median time to peak serum concentrations is 6 hours (range: 1.5 24 hours) following a single 4-g dose in healthy adults. 102 c The delayed-release granules (Paser ) contain an acid-resistant coating to protect against degradation in the stomach; the granules are designed to escape the usual restriction on gastric emptying of large particles. 102 The coating dissolves promptly (within 1 minute) at neutral pH such as that found in the small intestine or in neutral foods. 102 Distribution Extent Distributed into various tissues and fluids including peritoneal fluid, pleural fluid, and synovial fluid in concentrations approximately equal to plasma concentrations. a Also distributed into bile in low concentrations. a Distributed into CSF in low concentrations. 104 In patients with inflamed meninges, CSF concentrations are 10 50% of concurrent plasma concentrations. 104 Not known whether aminosalicylic acid crosses the placenta. a Distributed into milk in low concentrations. 102 Plasma Protein Binding 50 60%. 102 Elimination Metabolism Inactivated in the intestinal mucosa and liver primarily by acetylation. a Major metabolites are N -acetyl- p -aminosalicylic acid and p -aminosalicyluric acid. a The degree of metabolism is concentration-dependent and capacity-limited; the larger the dose absorbed, the lower the percentage of drug metabolized. a Elimination Route Aminosalicylic acid and its metabolites are excreted in urine by glomerular filtration and tubular secretion. a Approximately 77% of a dose is excreted in urine within 24 hours; 56% is excreted as the acetylated metabolite. a Aminosalicylic acid and the acetyl metabolite are removed by hemodialysis. 112 Half-life 1.5 hours (range 0.55 1.95 hours). c Special Populations Aminosalicylic acid and its acetyl metabolite accumulate in patients with severe renal impairment. 102 Continued acetylation of the parent drug leads exclusively to accumulation of the inactive acetylated form; deacetylation, if it occurs, is minor. 102 Stability Storage Oral Delayed-release Granules <15 C (i.e., in a refrigerator or freezer) prior to dispensing. 102 After dispensing, store in a refrigerator or freezer; may be stored at room temperature for short periods of time. 102 Avoid exposure to excessive heat, moisture, or light. 102 a Do not use if the airtight package containing the granules is swollen. 102 Do not use if the granules have lost their tan color and are turning dark brown or purple. 102 Actions and Spectrum Bacteriostatic in action. 102 Mechanism of action is similar to that of sulfonamides. a Aminosalicylic acid prevents synthesis of folic acid in susceptible organisms by competitively blocking conversion of aminobenzoic acid to dihydrofolic acid. a Highly specific antibacterial agent; active only against M. tuberculosis . a Inactive against M. avium complex (MAC) and other mycobacteria. a Natural and acquired resistance to aminosalicylic acid demonstrated in vitro and in vivo. 111 a No evidence of cross-resistance between aminosalicylic acid and other antituberculosis agents currently available in the US. a Advice to Patients Advise patients that poor compliance with antituberculosis regimens can result in treatment failure and development of drug-resistant TB, which can be life-threatening and lead to other serious health risks. 102 104 Advise patients to take the drug as prescribed. 102 Importance of sprinkling it on acidic food (e.g., applesauce, yogurt) or suspending it in a fruit drink (e.g., tomato, orange, grapefruit, grape, cranberry, or apple juice, fruit punch ) to protect the coating of the drug. 102 Importance of storing the packets containing the delayed-release granules in a refrigerator or freezer; the drug should be stored at room temperature only for short periods of time. 102 Importance of not using the packet of delayed-release granules if the packet is swollen or if the granules have lost their tan color and are dark brown or purple. 102 Advise patients to inform their clinicians or pharmacist about such packets and to return the medication. 102 Advise patients that skeletons of the delayed-release granules (Paser ) may be seen in the stool. 102 Importance of immediately discontinuing the drug at the first signs of hypersensitivity (e.g., rash, fever, anorexia, nausea, diarrhea) and contacting their clinicians. 102 Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs, as well as any concomitant illnesses. 102 Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. 102 Importance of informing patients of other important precautionary information. 102 (See Cautions.) 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. Aminosalicylic Acid Routes Dosage Forms Strengths Brand Names Manufacturer Oral Granules, delayed-release (enteric-coated) 4 g/packet Paser Jacobus AHFS DI Essentials. Copyright 2017, Selected Revisions February 1, 2008. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814. Use is not currently included in the labeling approved by the US Food and Drug Administration. References Only references cited for selected revisions after 1984 are available electronically. 100. Hooymans PM, Merkus FWHM. Current status of cardiac glycoside drug interactions. Clin Pharm . 1985; 4:404-13. [PubMed 2412751] 101. Brown DD, Juhl RP, Warner SL. Decreased bioavailability of digoxin due to hypocholesterolemic interventions. Circulation . 1978; 58:164-72. [PubMed 647881] 102. Jacobus Pharmaceutical Co. Paser granules (aminosalicylic acid granules) prescribing information. Princeton, NJ; 1996 Jul. 103. Food and Drug Administration. Orphan designations pursuant to Section 526 of the Federal Food and Cosmetic Act as amended by the Orphan Drug Act (P.L. 97-414), to June 28, 1996. Rockville, MD; 1996 Jul. 104. Centers for Disease Control and Prevention. Treatment of tuberculosis, American Thoracic Society, CDC, and Infectious Diseases Society of America. MMWR Recomm Rep . 2003; 52(RR-11):1-77. 105. Hanauer SB. Inflammatory bowel disease. N Engl J Med . 1996; 334:841-8. [PubMed 8596552] 106. Podolsky DK. Inflammatory Bowel Disease. N Engl J Med . 2002; 347:417-29. [PubMed 12167685] 107. American Academy of Pediatrics. 2006 Red Book: Report of the Committee on Infectious Diseases. 27th ed. Elk Grove Village, IL: American Academy of Pediatrics; 2006. 108. Baumgart DC, Sandborn WJ. Inflammatory bowel disease: clinical aspects and established and evolving therapies. Lancet . 2007; 369:1641-57. [PubMed 17499606] 109. Peloquin CA, Berning SE, Huitt GA et al. Once-daily and twice-daily dosing of p-aminosalicylic acid granules. Am J Respir Crit Care Med . 1999; 159:932-4. [PubMed 10051275] 110. Wilson JW, Kelkar P, Frigas E. Para-aminosalicylic acid (PAS) desensitization review in a case of multidrug-resistant pulmonary tuberculosis. Int J Tuberc Lung Dis . 2003; 7:493-7. [PubMed 12757053] 111. Rengarajan J, Sassetti CM, Naroditskaya V et al. The folate pathway is a target for resistance to the drug para-aminosalicylic acid (PAS) in mycobacteria. Mol Microbiol . 2004; 53:275-82. [PubMed 15225321] 112. Malone RS, Fish DN, Spiegel DM et al. The effect of hemodialysis on cycloserine, ethionamide, para-aminosalicylate, and clofazimine. Chest . 1999; 116:984-90. [PubMed 10531163] a. AHFS Drug Information 2007. McEvoy GK, ed. Aminosalicylic Acid. American Society of Health-System Pharmacists; 2007:544-6. b. AHFS Drug Information 2007. McEvoy GK, ed. Antituberculosis Agents General Statement. American Society of Health-System Pharmacists; 2007:534-44. c. Peloquin CA, Henshaw TL, Huitt GA et al. Pharmacokinetic evaluation of para -aminosalicylic acid granules. Pharmacotherapy . 1994; 14:40-6. [PubMed 8159600] Next Interactions Print this page Add to My Med List More about aminosalicylic acid Side Effects During Pregnancy or Breastfeeding Drug Interactions Support Group 0 Reviews Add your own review/rating Drug class: aminosalicylates Consumer resources Aminosalicylic Acid Aminosalicylate sodium (Advanced Reading) Professional resources Aminosalicylic Acid (Wolters Kluwer) Other brands: Paser Related treatment guides Tuberculosis, Active Tuberculosis, Resistant> ]} FEATURED: CAR-T Cell Therapy Overview Mechanism of Action KTE-C19 Studies KTE-C19 Cancer Targets Adverse Events Manufacturing Drug Status Rx Availability Prescription only C Pregnancy Category Risk cannot be ruled out N/A CSA Schedule Not a controlled drug Approval History Drug history at FDA Drug Class Aminosalicylates Related Drugs Tuberculosis, Resistant bedaquiline , Paser , More... 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