Each Asacol HD delayed-release tablet for oral administration contains 800 mg of mesalamine, an antiinflammatory drug. Asacol HD delayed-release tablets have an outer protective coat consisting of a combination of acrylic based resins, Eudragit S (methacrylic acid copolymer B, NF) and Eudragit L (methacrylic acid copolymer A, NF). The inner coat consists of an acrylic based resin, Eudragit S, which dissolves at pH 7 or greater, releasing mesalamine in the terminal ileum and beyond for topical anti-inflammatory action in the colon. Mesalamine (also referred to as 5-aminosalicylic acid or 5-ASA) has the chemical name 5-amino-2-hydroxybenzoic acid; its structural formula is: Molecular Weight : 153.1
Molecular Formula : C7H7NO3 Inactive Ingredients: Each tablet contains colloidal silicon dioxide, dibutyl phthalate, edible black ink, ferric oxide red, ferric oxide yellow, lactose monohydrate, magnesium stearate, methacrylic acid copolymer B (Eudragit S), methacrylic acid copolymer A (Eudragit L), polyethylene glycol, povidone, sodium starch glycolate, and talc.

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The most serious adverse reactions seen in Asacol HD clinical trials or with other products that contain or are metabolized to mesalamine were:

• Renal impairment, including renal failure (rare) [see WARNINGS AND PRECAUTIONS]
• Acute exacerbation of colitis [see WARNINGS AND PRECAUTIONS]
• Hypersensitivity reactions [see WARNINGS AND PRECAUTIONS]

Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Asacol HD (mesalamine delayed-release tablets, oral) has been evaluated in 896 patients with ulcerative colitis in controlled studies. Three six-week, active-controlled studies were conducted comparing Asacol HD 4.8 g/day with Asacol (mesalamine) 2.4 g/day as control in patients with mildly to moderately active ulcerative colitis. In these studies, 727 patients were dosed with the Asacol HD (mesalamine delayed-release tablets, oral) tablet and 732 patients were dosed with the Asacol 400 mg tablet. (One Asacol HD (mesalamine delayed-release tablets, oral) 800 mg tablet has not been shown to be bioequivalent to two Asacol 400 mg tablets [see CLINICAL PHARMACOLOGY].) The most common reactions reported in the Asacol HD (mesalamine delayed-release tablets, oral) group were headache (4.7%), nausea (2.8%), nasopharyngitis (2.5%), abdominal pain (2.3%), exacerbation of ulcerative colitis (2.3%), diarrhea (1.7%), and dyspepsia (1.7%); Table 1 enumerates adverse drug reactions that occurred in the three studies. The most common reactions in the primary efficacy population of patients with moderately active ulcerative colitis (602 patients dosed with Asacol HD (mesalamine delayed-release tablets, oral) and 618 patients dosed with the Asacol 400 mg tablet) were the same as all treated patients. The majority of adverse reactions with Asacol HD (mesalamine delayed-release tablets, oral) in the double-blind, active-controlled trials were mild or moderate in severity and were reversible. Discontinuations due to adverse reactions occurred in 3.9% of patients in the Asacol HD (mesalamine delayed-release tablets, oral) group and in 4.2% of patients in the Asacol 400 mg tablet comparator group. The most common cause for discontinuation was gastrointestinal symptoms associated with ulcerative colitis. Severe adverse reactions occurred in 7.6% of patients in the Asacol HD (mesalamine delayed-release tablets, oral) group and in 7.6% of patients in the Asacol 400 mg tablet comparator group. Most of these reactions were gastrointestinal symptoms related to ulcerative colitis. Serious adverse reactions occurred in 0.8% of patients in the Asacol HD (mesalamine delayed-release tablets, oral) group and in 1.8% of patients in the Asacol 400 mg tablet comparator group. The majority involved the gastrointestinal system. Table 1 : Adverse Reactions Occurring in 1% or More of All Treated Patients (Three studies combined; Intent-to-treat population)
MedDRA Preferred Term Asacol*
2.4 g/day
(400 mg Tablet)
(N=732) Asacol HD (mesalamine delayed-release tablets, oral) *
4.8 g/day
(800 mg Tablet)
(N=727) Headache 4.9 % 4.7 % Nausea 2.9 % 2.8 % Nasopharyngitis 1.4 % 2.5 % Abdominal pain 2.3 % 2.3 % Ulcerative Colitis 2.7 % 2.3 % Diarrhea 1.9 % 1.7 % Dyspepsia 0.8 % 1.7 % Vomiting 1.6 % 1.4 % Flatulence 0.7 % 1.2 % Influenza 1.2 % 1.0 % Pyrexia 1.2 % 0.7 % Cough 1.4 % 0.3 % N = number of patients within specified treatment group
% =percentage of patients in category and treatment group
*One Asacol HD (mesalamine delayed-release tablets, oral) 800 mg tablet has not been shown to be bioequivalent to two Asacol 400 mg tablets [see CLINICAL PHARMACOLOGY]. Adverse Reaction Information from Other Sources In addition to the adverse reactions reported above in clinical trials involving the Asacol HD (mesalamine delayed-release tablets, oral) tablet, the adverse events listed below have been reported in controlled clinical trials, open label studies, literature reports, or foreign and domestic marketing experience with Asacol 400 mg tablets or other products that contain or are metabolized to mesalamine. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Body as a Whole: Facial edema, edema, peripheral edema, asthenia, chills, infection, malaise, pain, neck pain, chest pain, back pain, abdominal enlargement, lupus-like syndrome, drug fever (rare). Cardiovascular: Pericarditis (rare), pericardial effusion, myocarditis (rare), vasodilation, migraine. Gastrointestinal: Dry mouth, stomatitis, oral ulcers, anorexia, increased appetite, eructation, pancreatitis, cholecystitis, gastritis, gastroenteritis, gastrointestinal bleeding, perforated peptic ulcer (rare), constipation, hemorrhoids, rectal hemorrhage, bloody diarrhea, tenesmus, stool abnormality. Hepatic: There have been rare reports of hepatotoxicity, including jaundice, cholestatic jaundice, hepatitis, and possible hepatocellular damage including liver necrosis and liver failure. Some of these cases were fatal. Asymptomatic elevations of liver enzymes which usually resolve during continued use or with discontinuation of the drug have also been reported. One case of Kawasaki-like syndrome, that included changes in liver enzymes, was also reported. Hematologic: Agranulocytosis (rare), aplastic anemia (rare), anemia, thrombocytopenia, leukopenia, eosinophilia, lymphadenopathy. Musculoskeletal: Gout, rheumatoid arthritis, arthritis, arthralgia, joint disorder, myalgia, hypertonia. Neurological/Psychiatric: Anxiety, depression, somnolence, insomnia, nervousness, confusion, emotional lability, dizziness, vertigo, tremor, paresthesia, hyperesthesia, peripheral neuropathy (rare), Guillain-Barré syndrome (rare), and transverse myelitis (rare). Respiratory/Pulmonary: Sinusitis, rhinitis, pharyngitis, asthma exacerbation, pleuritis, bronchitis, eosinophilic pneumonia, interstitial pneumonitis. Skin: Alopecia, psoriasis (rare), pyoderma gangrenosum (rare), erythema nodosum, acne, dry skin, sweating, pruritus, urticaria, rash. Special Senses: Ear pain, tinnitus, ear congestion, ear disorder, conjunctivitis, eye pain, blurred vision, vision abnormality, taste perversion. Renal/Urogenital: Renal failure (rare), interstitial nephritis, minimal change nephropathy [see WARNINGS AND PRECAUTIONS], dysuria, urinary frequency and urgency, hematuria, epididymitis, decreased libido, dysmenorrhea, menorrhagia. Laboratory Abnormalities Elevated AST (SGOT) or ALT (SGPT), elevated alkaline phosphatase, elevated GGT, elevated LDH, elevated bilirubin, elevated serum creatinine and BUN. Read the Asacol HD (mesalamine delayed-release tablets, oral) Side Effects Center for a complete guide to possible side effectsLearn More »

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For the treatment of moderately active ulcerative colitis, the recommended dose of Asacol HD (mesalamine delayed-release tablets, oral) in adults is two 800 mg tablets to be taken three times daily with or without food, for a total daily dose of 4.8 g, for a duration of 6 weeks. Asacol HD (mesalamine delayed-release tablets, oral) use beyond 6 weeks has not been evaluated. Asacol HD (mesalamine delayed-release tablets, oral) should be swallowed whole without cutting, breaking, or chewing. One Asacol HD (mesalamine delayed-release tablets, oral) 800 mg tablet has not been shown to be bioequivalent to two Asacol 400 mg tablets [see CLINICAL PHARMACOLOGY].

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No formal drug interaction studies have been performed using Asacol HD (mesalamine delayed-release tablets, oral) with other drugs. Last reviewed on RxList: 10/23/2009
This monograph has been modified to include the generic and brand name in many instances.

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Asacol HD (mesalamine delayed-release tablets, oral) is indicated for the treatment of moderately active ulcerative colitis. Safety and effectiveness of Asacol HD (mesalamine delayed-release tablets, oral) beyond 6 weeks has not been established.

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Asacol HD (mesalamine delayed-release tablets, oral) is contraindicated in patients with hypersensitivity to salicylates or aminosalicylates or to any of the components of Asacol HD (mesalamine delayed-release tablets, oral) tablets. Last reviewed on RxList: 10/23/2009
This monograph has been modified to include the generic and brand name in many instances.

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There is no specific antidote for mesalamine overdose and treatment for suspected acute severe toxicity with Asacol HD (mesalamine delayed-release tablets, oral) should be symptomatic and supportive. This may include prevention of further gastrointestinal tract absorption, correction of fluid electrolyte imbalance, and maintaining adequate renal function. Asacol HD (mesalamine delayed-release tablets, oral) is a pH dependent delayed release product and this factor should be considered when treating a suspected overdose. Single oral doses of 5000 mg/kg mesalamine suspension in mice (approximately 4.2 times the recommended human dose of Asacol HD (mesalamine delayed-release tablets, oral) based on body surface area), 4595 mg/kg in rats (approximately 7.8 times the recommended human dose of Asacol HD (mesalamine delayed-release tablets, oral) based on body surface area) and 3000 mg/kg in cynomolgus monkeys (approximately 10 times the recommended human dose of Asacol HD based on body surface area) were lethal.

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Dosage Forms And Strengths Asacol HD (mesalamine delayed-release tablets, oral) delayed-release tablets are available as red-brown, capsule-shaped tablets containing 800 mg mesalamine and imprinted with “PG 800” in black. Storage And Handling Asacol HD tablets are available as red-brown, capsule-shaped tablets containing 800 mg mesalamine and imprinted with “PG 800” in black. NDC 0149-0783-01 Bottle of 180 Store at controlled room temperature 20° to 25°C (68° to 77°F) [See USP]. Procter & Gamble Pharmaceuticals, Inc., Cincinnati, OH 45202, under license from Medeva Pharma Suisse AG. Made in Germany, D-64331 Weiterstadt. Last reviewed on RxList: 10/23/2009
This monograph has been modified to include the generic and brand name in many instances.

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Renal Impairment Renal impairment, including minimal change nephropathy, acute and chronic interstitial nephritis, and, rarely, renal failure, has been reported in patients taking products such as Asacol HD that contain or are converted to mesalamine. It is recommended that all patients have an evaluation of renal function prior to initiation of Asacol HD (mesalamine delayed-release tablets, oral) and periodically while on therapy. Exercise caution when using Asacol HD (mesalamine delayed-release tablets, oral) in patients with known renal dysfunction or history of renal disease. In animal studies (rats, mice, dogs), the kidney was the principal organ for toxicity [see Nonclinical Toxicology]. Exacerbation of Ulcerative Colitis Symptoms Exacerbation of the symptoms of colitis has been reported in 2.3% of Asacol HD (mesalamine delayed-release tablets, oral) -treated 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 HD tablets as well as other mesalamine products. Symptoms usually abate when Asacol HD (mesalamine delayed-release tablets, oral) tablets are discontinued. Hypersensitivity Some patients who have experienced a hypersensitivity reaction to sulfasalazine may have a similar reaction to Asacol HD tablets or to other compounds that contain or are converted to mesalamine. Pyloric Stenosis Patients with pyloric stenosis may have prolonged gastric retention of Asacol HD tablets, which could delay release of mesalamine in the colon. Use in Hepatic Impairment There have been reports of hepatic failure in patients with pre-existing liver disease who have been administered mesalamine. Caution should be exercised when administering Asacol HD (mesalamine delayed-release tablets, oral) to patients with liver disease. Nonclinical Toxicology Carcinogenesis, Mutagenesis, Impairment of Fertility Dietary mesalamine was not carcinogenic in rats at doses as high as 480 mg/kg/day, or in mice at 2000 mg/kg/day. These doses are approximately 0.8 and 1.7 times the 4.8 g/day Asacol HD dose (based on body surface area). Mesalamine was not genotoxic in the Ames test, the Chinese hamster ovary cell chromosomal aberration assay, and the mouse micronucleus test. Mesalamine, at oral doses up to 480 mg/kg/day (about 0.8 times the recommended human treatment dose based on body surface area), was found to have no effect on fertility or reproductive performance of male and female rats. Use In Specific Populations Pregnancy Pregnancy Category B: Reproduction studies have been performed in rats at oral doses up to 480 mg/kg/day (about 0.8 times the recommended human treatment dose of 4.8 g/day based on body surface area) and rabbits at oral doses up to 480 mg/kg/day (about 1.6 times the recommended human treatment dose of 4.8 g/day based on body surface area) and have revealed no evidence of impaired fertility or harm to the fetus due to mesalamine. 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. Mesalamine is known to cross the placental barrier. Nursing Mothers Mesalamine and its N-acetyl metabolite have been detected in human breast milk. The clinical significance of this has not been determined. Caution should be exercised when Asacol HD (mesalamine delayed-release tablets, oral) is administered to a nursing woman. Pediatric Use Safety and effectiveness of Asacol HD (mesalamine delayed-release tablets, oral) in pediatric patients have not been established. Geriatric Use Clinical studies of Asacol HD (mesalamine delayed-release tablets, oral) did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently than younger subjects. Other reported clinical experience has not identified differences in response between the elderly and younger patients. In general, the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy in elderly patients should be considered when prescribing Asacol HD (mesalamine delayed-release tablets, oral) . Reports from uncontrolled clinical studies and postmarketing reporting systems for Asacol (mesalamine) suggested a higher incidence of blood dyscrasias, i.e., agranulocytosis, neutropenia, pancytopenia, in patients who were 65 years or older. Caution should be taken to closely monitor blood cell counts during mesalamine therapy. Mesalamine is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken when prescribing this drug therapy. It is recommended that all patients have an evaluation of renal function prior to initiation of Asacol HD therapy and periodically while on Asacol HD (mesalamine delayed-release tablets, oral) therapy [see WARNINGS AND PRECAUTIONS]. Last reviewed on RxList: 10/23/2009
This monograph has been modified to include the generic and brand name in many instances.

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