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Asacol (The Active Ingredient In Asacol, Mesalamine (5-aminosalicylic Ac)
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Pharmacology
The active ingredient in Asacol, mesalamine (5-aminosalicylic acid, also referred to as 5-ASA), is the major active component of sulfasalazine for the treatment of inflammatory bowel disease. The available evidence suggests that mesalamine has a topical anti-inflammatory effect on the colon, where it inhibits prostaglandin and leukotriene synthesis.
Asacol tablets have a special acrylic-based resin coating which does not allow the drug to be released below pH7. The coating delays release of mesalamine until the tablets reach the terminal ileum and colon. Once released in the colon, mesalamine is minimally absorbed and plasma levels are similar to those found following rectal administration of mesalamine. Approximately 20% of the administered dose released in the colon is absorbed, the remainder is available for colon therapeutic activity and excretion in the feces. The absorbed mesalamine is rapidly acetylated through the gut mucosal wall and by the liver. It is mainly excreted by the kidney, as N-acetyl-5-aminosalicylic acid.
Pharmacokinetics: Mesalamine release from Asacol is delayed until the terminal ileum as reflected by t max's of about 7hours for mesalamine and its metabolite, N-acetyl-5-ASA. The t 1/2 elim.'s were about 3hours for mesalamine and 10hours for N-acetyl-5-ASA.
Human studies conducted using radiological and serum markers showed that the Asacol coating delayed release of mesalamine until the terminal ileum was reached. Other studies compared mesalamine absorption when administered as an enema (a readily available dosage form) and when released for absorption in the stomach, small intestine, and colon relative to an i.v. dose. Once released in the colon, mesalamine was minimally absorbed and plasma levels were similar to those found following rectal administration. Approximately 20% of the administered dose released was absorbed, with about 80% available for topical activity in the colon. The absorbed mesalamine was rapidly acetylated through the gut mucosal wall and by the liver. It was mainly excreted by the kidney as N-acetyl-5-ASA.
Serum levels and urinary excretion of mesalamine and N-acetyl-5-ASA following single and multiple equimolar Asacol and sulfasalazine doses to healthy subjects and to patients were compared. There was no consistent trend for greater serum mesalamine or metabolite levels following Asacol dosage. Based on urinary dose recoveries, the extent of mesalamine absorption for Asacol was no greater than that for sulfasalazine. Overall, there were no meaningful differences in the extents of mesalamine absorption following equimolar Asacol and sulfasalazine doses.
In another study, there was a dose response in serum mesalamine and metabolite levels at Asacol doses of 1.2and 2.4g/day. In other studies when Asacol was administered at higher or lower doses than 1.2and 2.4g/day, serum mesalamine and N-acetyl-5-ASA concentrations differed from those for the 1.2and 2.4g/day doses as would be expected following a linear dose response relationship. The effects of coadministration of Asacol with cimetidine, an antacid containing activated simethicone and aluminum hydroxide, and antacid with a high fat meal were addressed in another study. There were no significant in vivo effects on mesalamine release or the extent of drug absorption from Asacol by any of the three treatments.
Clinical Trials: In a randomized, double-blind, placebo controlled clinical trial it was shown that Asacol (4.8g/day of mesalamine in divided doses) was highly effective in inducing remission in ulcerative colitis patients with active disease.
Additional double-blind clinical trials of 16-, 24-, and 52-weeks' duration have shown Asacol, in doses ranging from 0.8to 4.4g/day to be as effective as sulfasalazine for maintenance of remission. It is particularly noteworthy that most patients intolerant or allergic to sulfasalazine can be effectively maintained in remission on Asacol, as demonstrated in open-labeled clinical trials. In addition, male infertility resulting from sulfasalazine therapy has been shown to be reversible upon treatment with Asacol.
The active ingredient in Asacol, mesalamine (5-aminosalicylic acid, also referred to as 5-ASA), is the major active component of sulfasalazine for the treatment of inflammatory bowel disease. The available evidence suggests that mesalamine has a topical anti-inflammatory effect on the colon, where it inhibits prostaglandin and leukotriene synthesis.
Asacol tablets have a special acrylic-based resin coating which does not allow the drug to be released below pH7. The coating delays release of mesalamine until the tablets reach the terminal ileum and colon. Once released in the colon, mesalamine is minimally absorbed and plasma levels are similar to those found following rectal administration of mesalamine. Approximately 20% of the administered dose released in the colon is absorbed, the remainder is available for colon therapeutic activity and excretion in the feces. The absorbed mesalamine is rapidly acetylated through the gut mucosal wall and by the liver. It is mainly excreted by the kidney, as N-acetyl-5-aminosalicylic acid.
Pharmacokinetics: Mesalamine release from Asacol is delayed until the terminal ileum as reflected by t max's of about 7hours for mesalamine and its metabolite, N-acetyl-5-ASA. The t 1/2 elim.'s were about 3hours for mesalamine and 10hours for N-acetyl-5-ASA.
Human studies conducted using radiological and serum markers showed that the Asacol coating delayed release of mesalamine until the terminal ileum was reached. Other studies compared mesalamine absorption when administered as an enema (a readily available dosage form) and when released for absorption in the stomach, small intestine, and colon relative to an i.v. dose. Once released in the colon, mesalamine was minimally absorbed and plasma levels were similar to those found following rectal administration. Approximately 20% of the administered dose released was absorbed, with about 80% available for topical activity in the colon. The absorbed mesalamine was rapidly acetylated through the gut mucosal wall and by the liver. It was mainly excreted by the kidney as N-acetyl-5-ASA.
Serum levels and urinary excretion of mesalamine and N-acetyl-5-ASA following single and multiple equimolar Asacol and sulfasalazine doses to healthy subjects and to patients were compared. There was no consistent trend for greater serum mesalamine or metabolite levels following Asacol dosage. Based on urinary dose recoveries, the extent of mesalamine absorption for Asacol was no greater than that for sulfasalazine. Overall, there were no meaningful differences in the extents of mesalamine absorption following equimolar Asacol and sulfasalazine doses.
In another study, there was a dose response in serum mesalamine and metabolite levels at Asacol doses of 1.2and 2.4g/day. In other studies when Asacol was administered at higher or lower doses than 1.2and 2.4g/day, serum mesalamine and N-acetyl-5-ASA concentrations differed from those for the 1.2and 2.4g/day doses as would be expected following a linear dose response relationship. The effects of coadministration of Asacol with cimetidine, an antacid containing activated simethicone and aluminum hydroxide, and antacid with a high fat meal were addressed in another study. There were no significant in vivo effects on mesalamine release or the extent of drug absorption from Asacol by any of the three treatments.
Clinical Trials: In a randomized, double-blind, placebo controlled clinical trial it was shown that Asacol (4.8g/day of mesalamine in divided doses) was highly effective in inducing remission in ulcerative colitis patients with active disease.
Additional double-blind clinical trials of 16-, 24-, and 52-weeks' duration have shown Asacol, in doses ranging from 0.8to 4.4g/day to be as effective as sulfasalazine for maintenance of remission. It is particularly noteworthy that most patients intolerant or allergic to sulfasalazine can be effectively maintained in remission on Asacol, as demonstrated in open-labeled clinical trials. In addition, male infertility resulting from sulfasalazine therapy has been shown to be reversible upon treatment with Asacol.
Indications
The Active Ingredient In Asacol, Mesalamine (5-aminosalicylic Acid, Also Referred To As 5-ASA), Is The Major Active Component Of Sulfasalazine For The Treatment Of Inflammatory Bowel Disease. The Available Evidence Suggests That Mesalamine Has A Topical Anti-inflammatory Effect On The Colon, Where It Inhibits Prostaglandin And Leukotriene Synthesis.
Asacol Tablets Have A Special Acrylic-based Resin Coating Which Does Not Allow The Drug To Be Released Below PH7. The Coating Delays Release Of Mesalamine Until The Tablets Reach The Terminal Ileum And Colon. Once Released In The Colon, Mesalamine Is Minimally Absorbed And Plasma Levels Are Similar To Those Found Following Rectal Administration Of Mesalamine. Approximately 20% Of The Administered Dose Released In The Colon Is Absorbed, The Remainder Is Available For Colon Therapeutic Activity And Excretion In The Feces. The Absorbed Mesalamine Is Rapidly Acetylated Through The Gut Mucosal Wall And By The Liver. It Is Mainly Excreted By The Kidney, As N-acetyl-5-aminosalicylic Acid.
Pharmacokinetics: Mesalamine Release From Asacol Is Delayed Until The Terminal Ileum As Reflected By T Max's Of About 7hours For Mesalamine And Its Metabolite, N-acetyl-5-ASA. The T 1/2 Elim.'s Were About 3hours For Mesalamine And 10hours For N-acetyl-5-ASA.
Human Studies Conducted Using Radiological And Serum Markers Showed That The Asacol Coating Delayed Release Of Mesalamine Until The Terminal Ileum Was Reached. Other Studies Compared Mesalamine Absorption When Administered As An Enema (a Readily Available Dosage Form) And When Released For Absorption In The Stomach, Small Intestine, And Colon Relative To An I.v. Dose. Once Released In The Colon, Mesalamine Was Minimally Absorbed And Plasma Levels Were Similar To Those Found Following Rectal Administration. Approximately 20% Of The Administered Dose Released Was Absorbed, With About 80% Available For Topical Activity In The Colon. The Absorbed Mesalamine Was Rapidly Acetylated Through The Gut Mucosal Wall And By The Liver. It Was Mainly Excreted By The Kidney As N-acetyl-5-ASA.
Serum Levels And Urinary Excretion Of Mesalamine And N-acetyl-5-ASA Following Single And Multiple Equimolar Asacol And Sulfasalazine Doses To Healthy Subjects And To Patients Were Compared. There Was No Consistent Trend For Greater Serum Mesalamine Or Metabolite Levels Following Asacol Dosage. Based On Urinary Dose Recoveries, The Extent Of Mesalamine Absorption For Asacol Was No Greater Than That For Sulfasalazine. Overall, There Were No Meaningful Differences In The Extents Of Mesalamine Absorption Following Equimolar Asacol And Sulfasalazine Doses.
In Another Study, There Was A Dose Response In Serum Mesalamine And Metabolite Levels At Asacol Doses Of 1.2and 2.4g/day. In Other Studies When Asacol Was Administered At Higher Or Lower Doses Than 1.2and 2.4g/day, Serum Mesalamine And N-acetyl-5-ASA Concentrations Differed From Those For The 1.2and 2.4g/day Doses As Would Be Expected Following A Linear Dose Response Relationship. The Effects Of Coadministration Of Asacol With Cimetidine, An Antacid Containing Activated Simethicone And Aluminum Hydroxide, And Antacid With A High Fat Meal Were Addressed In Another Study. There Were No Significant In Vivo Effects On Mesalamine Release Or The Extent Of Drug Absorption From Asacol By Any Of The Three Treatments.
Clinical Trials: In A Randomized, Double-blind, Placebo Controlled Clinical Trial It Was Shown That Asacol (4.8g/day Of Mesalamine In Divided Doses) Was Highly Effective In Inducing Remission In Ulcerative Colitis Patients With Active Disease.
Additional Double-blind Clinical Trials Of 16-, 24-, And 52-weeks' Duration Have Shown Asacol, In Doses Ranging From 0.8to 4.4g/day To Be As Effective As Sulfasalazine For Maintenance Of Remission. It Is Particularly Noteworthy That Most Patients Intolerant Or Allergic To Sulfasalazine Can Be Effectively Maintained In Remission On Asacol, As Demonstrated In Open-labeled Clinical Trials. In Addition, Male Infertility Resulting From Sulfasalazine Therapy Has Been Shown To Be Reversible Upon Treatment With Asacol.
The Active Ingredient In Asacol, Mesalamine (5-aminosalicylic Acid, Also Referred To As 5-ASA), Is The Major Active Component Of Sulfasalazine For The Treatment Of Inflammatory Bowel Disease. The Available Evidence Suggests That Mesalamine Has A Topical Anti-inflammatory Effect On The Colon, Where It Inhibits Prostaglandin And Leukotriene Synthesis.
Asacol Tablets Have A Special Acrylic-based Resin Coating Which Does Not Allow The Drug To Be Released Below PH7. The Coating Delays Release Of Mesalamine Until The Tablets Reach The Terminal Ileum And Colon. Once Released In The Colon, Mesalamine Is Minimally Absorbed And Plasma Levels Are Similar To Those Found Following Rectal Administration Of Mesalamine. Approximately 20% Of The Administered Dose Released In The Colon Is Absorbed, The Remainder Is Available For Colon Therapeutic Activity And Excretion In The Feces. The Absorbed Mesalamine Is Rapidly Acetylated Through The Gut Mucosal Wall And By The Liver. It Is Mainly Excreted By The Kidney, As N-acetyl-5-aminosalicylic Acid.
Pharmacokinetics: Mesalamine Release From Asacol Is Delayed Until The Terminal Ileum As Reflected By T Max's Of About 7hours For Mesalamine And Its Metabolite, N-acetyl-5-ASA. The T 1/2 Elim.'s Were About 3hours For Mesalamine And 10hours For N-acetyl-5-ASA.
Human Studies Conducted Using Radiological And Serum Markers Showed That The Asacol Coating Delayed Release Of Mesalamine Until The Terminal Ileum Was Reached. Other Studies Compared Mesalamine Absorption When Administered As An Enema (a Readily Available Dosage Form) And When Released For Absorption In The Stomach, Small Intestine, And Colon Relative To An I.v. Dose. Once Released In The Colon, Mesalamine Was Minimally Absorbed And Plasma Levels Were Similar To Those Found Following Rectal Administration. Approximately 20% Of The Administered Dose Released Was Absorbed, With About 80% Available For Topical Activity In The Colon. The Absorbed Mesalamine Was Rapidly Acetylated Through The Gut Mucosal Wall And By The Liver. It Was Mainly Excreted By The Kidney As N-acetyl-5-ASA.
Serum Levels And Urinary Excretion Of Mesalamine And N-acetyl-5-ASA Following Single And Multiple Equimolar Asacol And Sulfasalazine Doses To Healthy Subjects And To Patients Were Compared. There Was No Consistent Trend For Greater Serum Mesalamine Or Metabolite Levels Following Asacol Dosage. Based On Urinary Dose Recoveries, The Extent Of Mesalamine Absorption For Asacol Was No Greater Than That For Sulfasalazine. Overall, There Were No Meaningful Differences In The Extents Of Mesalamine Absorption Following Equimolar Asacol And Sulfasalazine Doses.
In Another Study, There Was A Dose Response In Serum Mesalamine And Metabolite Levels At Asacol Doses Of 1.2and 2.4g/day. In Other Studies When Asacol Was Administered At Higher Or Lower Doses Than 1.2and 2.4g/day, Serum Mesalamine And N-acetyl-5-ASA Concentrations Differed From Those For The 1.2and 2.4g/day Doses As Would Be Expected Following A Linear Dose Response Relationship. The Effects Of Coadministration Of Asacol With Cimetidine, An Antacid Containing Activated Simethicone And Aluminum Hydroxide, And Antacid With A High Fat Meal Were Addressed In Another Study. There Were No Significant In Vivo Effects On Mesalamine Release Or The Extent Of Drug Absorption From Asacol By Any Of The Three Treatments.
Clinical Trials: In A Randomized, Double-blind, Placebo Controlled Clinical Trial It Was Shown That Asacol (4.8g/day Of Mesalamine In Divided Doses) Was Highly Effective In Inducing Remission In Ulcerative Colitis Patients With Active Disease.
Additional Double-blind Clinical Trials Of 16-, 24-, And 52-weeks' Duration Have Shown Asacol, In Doses Ranging From 0.8to 4.4g/day To Be As Effective As Sulfasalazine For Maintenance Of Remission. It Is Particularly Noteworthy That Most Patients Intolerant Or Allergic To Sulfasalazine Can Be Effectively Maintained In Remission On Asacol, As Demonstrated In Open-labeled Clinical Trials. In Addition, Male Infertility Resulting From Sulfasalazine Therapy Has Been Shown To Be Reversible Upon Treatment With Asacol.
Contraindications
In patients with a history of sensitivity to salicylates; existing gastric or duodenal ulcer; urinary tract obstruction; and in infants under 2years of age.
In patients with a history of sensitivity to salicylates; existing gastric or duodenal ulcer; urinary tract obstruction; and in infants under 2years of age.
Safety Information / Warning
If toxic or hypersensitivity reactions occur, the drug should be discontinued. In assessing liver and joint complications, it should be kept in mind that these are frequently associated with ulcerative colitis.
If toxic or hypersensitivity reactions occur, the drug should be discontinued. In assessing liver and joint complications, it should be kept in mind that these are frequently associated with ulcerative colitis.
Precautions
General: Patients with pyloric stenosis may have prolonged gastric retention of Asacol tablets which could delay release of mesalamine in the colon.
Exacerbation of the symptoms of colitis, thought to have been caused by mesalamine or sulfasalazine has been reported in 3% of patients in controlled clinical trials. This acute reaction, characterized by cramping, abdominal pain, bloody diarrhea, and occasionally by fever, headache, malaise, pruritus, rash and conjunctivitis, has been reported after the initiation of Asacol tablets as well as other mesalamine products. Symptoms usually abate when Asacol tablets are discontinued.
Renal: Renal impairment, including minimal change nephropathy, and acute and chronic interstitial nephritis, has been reported in patients taking Asacol tablets as well as in patients taking other mesalamine products.
Caution should be exercised in patients with impaired renal function and/or hepatic dysfunction. It is recommended that all patients have an evaluation of renal function prior to initiation of Asacol tablets and periodically while on Asacol therapy.
Drug Interactions : There are no known drug interactions. The effects of coadministration of Asacol with cimetidine, with an antacid containing activated dimethicone and aluminum hydroxide, or with an antacid accompanied by a high fat meal were addressed in a clinical study. There were no significant in vivo effects on mesalamine release or the extent of drug absorption from Asacol by any of the 3treatments. It has been reported that simultaneous administration of famotidine, a potent H 2-antagonist, and Asacol does not influence the absorption and urinary excretion of mesalamine.
Asacol should not be administered with preparations which lower the stool pH, such as lactulose.
Interactions similar to ASA cannot be excluded.
Pregnancy: In reproduction studies, mesalamine was administered orally at a dosage of480mg/kg/day to pregnant rats and rabbits. No evidence of impaired female fertility or harm to the fetus due to therapy with Asacol was observed. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
Lactation: It has been reported that small amounts of5-ASA and higher concentrations of acetyl-5-ASA are found in breast milk. While clinical significance of this has not been determined, caution should be exercised when Asacol is administered to a nursing woman.
Children: Safety and effectiveness of Asacol therapy in children have not been established.
Information to Be Provided to the Patient: 1.Swallow tablets whole, taking care not to break the outer coating. The outer coating is designed to remain intact, to protect the active ingredient until it reaches the terminal ileum, where the tablet coating dissolves and the contents of the tablet are released into the terminal ileum and colon.
2.Take Asacol tablets only as prescribed. Do not change the number or frequency of tablets ingested without first consulting your physician.
3.What appears to be intact or partially intact tablets may infrequently appear in the stool. If this occurs repeatedly, consult your physician.
General: Patients with pyloric stenosis may have prolonged gastric retention of Asacol tablets which could delay release of mesalamine in the colon.
Exacerbation of the symptoms of colitis, thought to have been caused by mesalamine or sulfasalazine has been reported in 3% of patients in controlled clinical trials. This acute reaction, characterized by cramping, abdominal pain, bloody diarrhea, and occasionally by fever, headache, malaise, pruritus, rash and conjunctivitis, has been reported after the initiation of Asacol tablets as well as other mesalamine products. Symptoms usually abate when Asacol tablets are discontinued.
Renal: Renal impairment, including minimal change nephropathy, and acute and chronic interstitial nephritis, has been reported in patients taking Asacol tablets as well as in patients taking other mesalamine products.
Caution should be exercised in patients with impaired renal function and/or hepatic dysfunction. It is recommended that all patients have an evaluation of renal function prior to initiation of Asacol tablets and periodically while on Asacol therapy.
Drug Interactions : There are no known drug interactions. The effects of coadministration of Asacol with cimetidine, with an antacid containing activated dimethicone and aluminum hydroxide, or with an antacid accompanied by a high fat meal were addressed in a clinical study. There were no significant in vivo effects on mesalamine release or the extent of drug absorption from Asacol by any of the 3treatments. It has been reported that simultaneous administration of famotidine, a potent H 2-antagonist, and Asacol does not influence the absorption and urinary excretion of mesalamine.
Asacol should not be administered with preparations which lower the stool pH, such as lactulose.
Interactions similar to ASA cannot be excluded.
Pregnancy: In reproduction studies, mesalamine was administered orally at a dosage of480mg/kg/day to pregnant rats and rabbits. No evidence of impaired female fertility or harm to the fetus due to therapy with Asacol was observed. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
Lactation: It has been reported that small amounts of5-ASA and higher concentrations of acetyl-5-ASA are found in breast milk. While clinical significance of this has not been determined, caution should be exercised when Asacol is administered to a nursing woman.
Children: Safety and effectiveness of Asacol therapy in children have not been established.
Information to Be Provided to the Patient: 1.Swallow tablets whole, taking care not to break the outer coating. The outer coating is designed to remain intact, to protect the active ingredient until it reaches the terminal ileum, where the tablet coating dissolves and the contents of the tablet are released into the terminal ileum and colon.
2.Take Asacol tablets only as prescribed. Do not change the number or frequency of tablets ingested without first consulting your physician.
3.What appears to be intact or partially intact tablets may infrequently appear in the stool. If this occurs repeatedly, consult your physician.
Side Effects / Adverse Effects
Asacol is generally well tolerated. Adverse events seen in clinical trials with Asacol tablets have generally been mild and reversible, and have seldom resulted in discontinuation of treatment. Because Asacol does not contain a sulfa moiety, sulfa-related side effects are avoided. Many patients with a history of sulfasalazine intolerance are able to tolerate Asacol as demonstrated in open-label clinical trials. However, some patients who have experienced a hypersensitivity reaction to sulfasalazine may have a similar reaction to Asacol tablets or to other compounds which contain or are converted to mesalamine.
In 2 short-term (6weeks), double-blind, placebo-controlled clinical studies involving 245 patients, 155 of whom were randomized to Asacol tablets, 5 (3.2%) of the Asacol patients discontinued Asacol therapy because of adverse events as compared to 2 (2.2%) of the placebo patients. Adverse reactions leading to withdrawal from Asacol tablets include (each in 1 patient): diarrhea and colitis flare; dizziness, nausea, joint pain, and headache; rash, lethargy and constipation; dry mouth, malaise, lower back discomfort, mild disorientation, mild indigestion and cramping; headache, nausea, malaise, aching, vomiting, muscle cramps, a stuffy head, plugged ears, and fever.
Adverse events occurring at a frequency of greater than 2% in these clinical trials are listed below. Overall, the incidence of adverse events seen with Asacol tablets was similar to placebo.
Headache, abdominal pain, eructation, pain, nausea, pharyngitis, dizziness, asthenia, diarrhea, back pain, fever, rash, dyspepsia, rhinitis, arthralgia, vomiting, constipation, hypertonia, flatulence, flu syndrome, chills, colitis exacerbation, chest pain, peripheral edema, myalgia, pruritus, sweating, dysmenorrhea.
Of these adverse events, only rash showed a consistently higher frequency with increasing Asacol dose in these studies.
The following adverse reactions were seen in 2% of the patients in the controlled studies: malaise, arthritis, insomnia, increased cough, acne, and conjunctivitis.
In uncontrolled clinical studies, the following adverse events occured at a frequency of 5% or greater and appeared to increase in frequency with increasing dose: asthenia, flu syndrome, back pain, arthralgia, and rhinitis.
In addition to the adverse events listed above, the following adverse events have also been reported in controlled clinical trials, open-label studies, literature reports, or foreign and domestic marketing experience. Because many of these events were reported voluntarily from a population of unknown size, estimates of frequency cannot be made. The relationship of the reported events to Asacol is unclear in many cases, some, including anorexia, joint pain, pyoderma gangrenosum, oral ulcers, and anemia are sometimes part of the clinical presentation of ulcerative colitis.
Body as a Whole: neck pain, abdominal enlargement, facial edema, edema, lupus-like syndrome.
Cardiovascular: pericarditis (rare), myocarditis (rare), vasodilation, migraine.
Digestive: anorexia, hepatitis (rare), pancreatitis, gastroenteritis, gastritis, increased appetite, cholecystitis, dry mouth, oral ulcers, perforated peptic ulcer (rare), bloody diarrhea, tenesmus.
Hematologic: agranulocytosis (rare), aplastic anemia (rare), thrombocytopenia, eosinophilia, leukopenia, anemia, lymphadenopathy.
Musculoskeletal: gout.
Nervous: anxiety, depression, somnolence, emotional lability, hyperesthesia, vertigo, nervousness, confusion, paresthesia, tremor, peripheral neuropathy (rare), Guillain-Barré syndrome (rare), and transverse myelitis (rare).
Respiratory/Pulmonary: sinusitis, eosinophilic pneumonia, interstitial pneumonitis, asthma exacerbation, pleuritis.
Skin: alopecia, psoriasis (rare), pyoderma gangrenosum (rare), dry skin, erythema nodosum, urticaria.
Special Senses: ear pain, eye pain, taste perversion, blurred vision, tinnitus.
Urogenital: interstitial nephritis (see also Precautions), minimal change nephropathy (see also Precautions), dysuria, urinary urgency, hematuria, epididymitis, menorrhagia.
Laboratory Abnormalities: elevated AST or ALT, elevated alkaline phosphatase, elevated serum creatinine and BUN.
Hepatic: Asymptomatic elevations of liver function tests have occurred in patients taking Asacol tablets. These elevations usually resolve during continued therapy or with discontinuation of Asacol. When any elevations in liver enzymes are assessed, it should be kept in mind that hepatic complications are frequently associated with inflammatory bowel disease.
Asacol is generally well tolerated. Adverse events seen in clinical trials with Asacol tablets have generally been mild and reversible, and have seldom resulted in discontinuation of treatment. Because Asacol does not contain a sulfa moiety, sulfa-related side effects are avoided. Many patients with a history of sulfasalazine intolerance are able to tolerate Asacol as demonstrated in open-label clinical trials. However, some patients who have experienced a hypersensitivity reaction to sulfasalazine may have a similar reaction to Asacol tablets or to other compounds which contain or are converted to mesalamine.
In 2 short-term (6weeks), double-blind, placebo-controlled clinical studies involving 245 patients, 155 of whom were randomized to Asacol tablets, 5 (3.2%) of the Asacol patients discontinued Asacol therapy because of adverse events as compared to 2 (2.2%) of the placebo patients. Adverse reactions leading to withdrawal from Asacol tablets include (each in 1 patient): diarrhea and colitis flare; dizziness, nausea, joint pain, and headache; rash, lethargy and constipation; dry mouth, malaise, lower back discomfort, mild disorientation, mild indigestion and cramping; headache, nausea, malaise, aching, vomiting, muscle cramps, a stuffy head, plugged ears, and fever.
Adverse events occurring at a frequency of greater than 2% in these clinical trials are listed below. Overall, the incidence of adverse events seen with Asacol tablets was similar to placebo.
Headache, abdominal pain, eructation, pain, nausea, pharyngitis, dizziness, asthenia, diarrhea, back pain, fever, rash, dyspepsia, rhinitis, arthralgia, vomiting, constipation, hypertonia, flatulence, flu syndrome, chills, colitis exacerbation, chest pain, peripheral edema, myalgia, pruritus, sweating, dysmenorrhea.
Of these adverse events, only rash showed a consistently higher frequency with increasing Asacol dose in these studies.
The following adverse reactions were seen in 2% of the patients in the controlled studies: malaise, arthritis, insomnia, increased cough, acne, and conjunctivitis.
In uncontrolled clinical studies, the following adverse events occured at a frequency of 5% or greater and appeared to increase in frequency with increasing dose: asthenia, flu syndrome, back pain, arthralgia, and rhinitis.
In addition to the adverse events listed above, the following adverse events have also been reported in controlled clinical trials, open-label studies, literature reports, or foreign and domestic marketing experience. Because many of these events were reported voluntarily from a population of unknown size, estimates of frequency cannot be made. The relationship of the reported events to Asacol is unclear in many cases, some, including anorexia, joint pain, pyoderma gangrenosum, oral ulcers, and anemia are sometimes part of the clinical presentation of ulcerative colitis.
Body as a Whole: neck pain, abdominal enlargement, facial edema, edema, lupus-like syndrome.
Cardiovascular: pericarditis (rare), myocarditis (rare), vasodilation, migraine.
Digestive: anorexia, hepatitis (rare), pancreatitis, gastroenteritis, gastritis, increased appetite, cholecystitis, dry mouth, oral ulcers, perforated peptic ulcer (rare), bloody diarrhea, tenesmus.
Hematologic: agranulocytosis (rare), aplastic anemia (rare), thrombocytopenia, eosinophilia, leukopenia, anemia, lymphadenopathy.
Musculoskeletal: gout.
Nervous: anxiety, depression, somnolence, emotional lability, hyperesthesia, vertigo, nervousness, confusion, paresthesia, tremor, peripheral neuropathy (rare), Guillain-Barré syndrome (rare), and transverse myelitis (rare).
Respiratory/Pulmonary: sinusitis, eosinophilic pneumonia, interstitial pneumonitis, asthma exacerbation, pleuritis.
Skin: alopecia, psoriasis (rare), pyoderma gangrenosum (rare), dry skin, erythema nodosum, urticaria.
Special Senses: ear pain, eye pain, taste perversion, blurred vision, tinnitus.
Urogenital: interstitial nephritis (see also Precautions), minimal change nephropathy (see also Precautions), dysuria, urinary urgency, hematuria, epididymitis, menorrhagia.
Laboratory Abnormalities: elevated AST or ALT, elevated alkaline phosphatase, elevated serum creatinine and BUN.
Hepatic: Asymptomatic elevations of liver function tests have occurred in patients taking Asacol tablets. These elevations usually resolve during continued therapy or with discontinuation of Asacol. When any elevations in liver enzymes are assessed, it should be kept in mind that hepatic complications are frequently associated with inflammatory bowel disease.
Overdose
Symptoms and Treatment: Two cases of pediatric overdosage have been reported. A 3-year-old male ingested 2g of Asacol tablets. He was treated with ipecac and activated charcoal. No adverse events occurred. Another 3-year-old male, approximately 16kg, ingested an unknown amount of a maximum of 24g of Asacol crushed in solution (i.e., uncoated mesalamine). He was treated with orange juice and activated charcoal and experienced no adverse events. Mesalamine is not metabolized to salicylate. If the amount ingested is considered dangerous or excessive, induce vomiting with ipecac syrup unless the patient is convulsing, comatose, or has lost the gag reflex, in which case perform gastric lavage using a large bore tube. If indicated, follow with activated charcoal and a saline cathartic. There is no specific antidote and treatment is symptomatic and supportive.
Symptoms and Treatment: Two cases of pediatric overdosage have been reported. A 3-year-old male ingested 2g of Asacol tablets. He was treated with ipecac and activated charcoal. No adverse events occurred. Another 3-year-old male, approximately 16kg, ingested an unknown amount of a maximum of 24g of Asacol crushed in solution (i.e., uncoated mesalamine). He was treated with orange juice and activated charcoal and experienced no adverse events. Mesalamine is not metabolized to salicylate. If the amount ingested is considered dangerous or excessive, induce vomiting with ipecac syrup unless the patient is convulsing, comatose, or has lost the gag reflex, in which case perform gastric lavage using a large bore tube. If indicated, follow with activated charcoal and a saline cathartic. There is no specific antidote and treatment is symptomatic and supportive.
Recommended Dosage
Usual daily adult dose is 2to 8Asacol 400mg tablets, taken orally in divided doses. In patients with severe active disease, the dose may be increased to 12tablets daily. Abrupt discontinuation is not recommended. Prolonged treatment may be required.
Usual daily adult dose is 2to 8Asacol 400mg tablets, taken orally in divided doses. In patients with severe active disease, the dose may be increased to 12tablets daily. Abrupt discontinuation is not recommended. Prolonged treatment may be required.
Supplied / Packaging
Each brown-red, capsule-shaped, enteric-coated tablet contains: 5-ASA 400mg (mesalamine), coated with a special acrylic-based resin, EudragitS (methacrylic acid copolymer TypeB), which delays release of the 5-ASA until the tablet reaches the terminal ileum. Nonmedicinal ingredients: dibutyl phthalate, EudragitS (methacrylic acid copolymer TypeB [USP]), iron oxide red, iron oxide yellow, lactose, magnesium stearate, polyethylene glycol, polyvinylpyrrolidone, sodium starch glycolate and talc. Blister packs of10, cartons of10. Store at controlled room temperature (15to30°C).
Each brown-red, capsule-shaped, enteric-coated tablet contains: 5-ASA 400mg (mesalamine), coated with a special acrylic-based resin, EudragitS (methacrylic acid copolymer TypeB), which delays release of the 5-ASA until the tablet reaches the terminal ileum. Nonmedicinal ingredients: dibutyl phthalate, EudragitS (methacrylic acid copolymer TypeB [USP]), iron oxide red, iron oxide yellow, lactose, magnesium stearate, polyethylene glycol, polyvinylpyrrolidone, sodium starch glycolate and talc. Blister packs of10, cartons of10. Store at controlled room temperature (15to30°C).
