Mesalamine 800 mg Tablet, Delayed Release, 180-count
Other active recalls for Mesalamine (different manufacturers) — 1 · tap to view
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Aminosalicylate class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Mesalamine is used to treat ulcerative colitis (a condition which causes swelling and sores in the lining of the colon [large intestine] and rectum) and also to maintain improvement of ulcerative colitis symptoms. Mesalamine is in a class of medications called anti-inflammatory agents. It works by stopping the body from producing a certain substance that may cause inflammation.
Read the full MedlinePlus article ↗- Mesalamine works to reduce inflammation directly in the lining of your colon or rectum. Depending on which product you've been prescribed, it can help bring an active flare of ulce...
- What exactly is mesalamine supposed to do for me?
- It really does matter, and they're not interchangeable. The form your doctor chose depends on where in your bowel the inflammation is. Rectal suppositories (like CANASA) treat infl...
- There are so many different forms — pills, enemas, suppositories. Does it matter which one I use?
Patient education
Supplement & herbal interactions
Some supplements/herbs that may interact with Mesalamine — tap one for details:
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💊 What it looks like
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.
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UNII 4W5IH7FLNY
A clear, oily liquid derived from sebacic acid and butanol. It works as a plasticizer and solvent in pharmaceutical coatings and films, helping them stay flexible and smooth.
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UNII 1K09F3G675
Ferric oxide red is an inorganic iron compound used as a colorant in medicines. It gives tablets, capsules, or other dosage forms a red or reddish tint for identification and appearance.
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UNII EX438O2MRT
Ferric oxide yellow is a naturally occurring iron compound used as a colorant in medications. It gives tablets, capsules, and other forms a yellow or golden hue for identification and appearance.
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UNII XM0M87F357
A dark iron oxide compound that gives medicines their black or dark color. It's used as a colorant in tablets and capsules to help identify the product and make it visually distinctive.
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UNII 3NXW29V3WO
Hypromellose is a plant-based thickener made from cellulose. It's used in medicines as a binder to hold ingredients together, a coating for tablets, and a thickener for liquids.
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UNII EWQ57Q8I5X
Lactose monohydrate is a natural sugar derived from milk. It serves as a filler and binder in tablets and capsules, helping create the proper size, texture, and consistency of the medicine.
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UNII 70097M6I30
Magnesium stearate is a salt made from magnesium and stearic acid, a fatty substance. It's used in tablets and capsules as a lubricant and glidant to help ingredients flow smoothly during manufacturing and prevent sticking.
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UNII 5KY68S2577
A synthetic plastic polymer made from two chemical compounds combined in a specific ratio. It forms a coating on tablets and capsules to control how and where the medication dissolves in the digestive tract.
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UNII NX76LV5T8J
A synthetic plastic polymer made from methacrylic acid and ethyl acrylate. It's used as a coating or binder to control how and where the medicine dissolves in your digestive system.
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UNII 3WJQ0SDW1A
Polyethylene glycol is a synthetic liquid or solid polymer used in medicines as a solvent, lubricant, and humectant. It helps dissolve active ingredients, reduces friction during manufacturing, and retains moisture in the final product.
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UNII FZ989GH94E
Povidone is a synthetic polymer made from a plastic-like material. It acts as a binder to hold tablet ingredients together and as a disintegrant to help the tablet break apart in your stomach so the medicine can be absorbed.
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UNII 6DC9Q167V3
Propylene glycol is a clear liquid derived from petroleum or vegetable sources. It acts as a solvent, humectant, and preservative in medicines, helping dissolve active ingredients and maintain product stability.
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UNII 46N107B71O
Shellac is a natural resin secreted by the lac beetle. It's used as a coating on tablets and capsules to control how quickly the medicine dissolves and to improve appearance and stability.
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UNII ETJ7Z6XBU4
Silicon dioxide is a naturally occurring mineral used as a glidant and anti-caking agent. It helps powder ingredients flow smoothly and prevents clumping during manufacturing and storage.
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UNII 5856J3G2A2
A starch-based powder made from potatoes and processed with sodium. It acts as a disintegrant, helping the tablet or capsule break apart quickly in the stomach so the medicine can be absorbed.
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UNII 7SEV7J4R1U
A powder made from a naturally occurring mineral. In medicines, talc works as a glidant and anti-caking agent, helping tablets and capsules flow smoothly during manufacturing and preventing clumping.
16 inactive ingredients listed in the exact product block matched to this NDC.
Where does this data come from?
ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per ea | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $4.003 | $720.49 / 180 tablets |
| Medicaid paysCMS SDUD · 12 mo | $5.10 | $917.30 / 180 tablets |
| Medicare drug plans payPart D · Q2 2026 | $5.29 | $951.55 / 180 tablets |
Where does this data come from?
🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Mesalamine 800 mg 00480-7750-80 | Teva | 180 tablets | $4.003 | AB | Availability likely | — |
| Mesalamine 800 mg 60687-0408-25 | American | 1 tablet | $4.003 | AB | Availability likely | — |
| Mesalamine 800 mgthis 65162-0360-18 | Amneal | 180 tablets | $4.003 | AB | Availability likely | — |
| mesalamine 800 mg 68382-0435-28 | Zydus | 180 tablets | $4.003 | AB | Availability likely | — |
| Mesalamine 800 mg 42291-0489-18 | AvKARE | 180 tablets | — | AB | FDA listed | — |
| mesalamine 800 mg 70771-1110-04 | Zydus | 10 tablets | — | AB | FDA listed | — |
Where does this data come from?
⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
Where does this data come from?
🗺️ Medicaid utilization & spend
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 65162-0360-18 You're viewing this | 180 TABLET, DELAYED RELEASE in 1 BOTTLE (65162-360-18) | 2025-02-19 | Active |
📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Mesalamine delayed-release tablets are indicated for the treatment of moderately active ulcerative colitis in adults. Limitations of Use : Safety and effectiveness of mesalamine delayed-release tablets beyond 6 weeks have not been established. Mesalamine delayed-release tablets are an aminosalicylate indicated for the treatment of moderately active ulcerative colitis in adults.
(1) Limitation of Use : Safety and effectiveness of mesalamine delayed-release tablets beyond 6 weeks have not been established (1)
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Important Administration Instructions : Do not substitute one mesalamine delayed-release tablets 800 mg tablet for two mesalamine delayed-release 400 mg oral products. (2.1) Evaluate renal function prior to initiation of mesalamine delayed-release tablets. (2.1, 5.1) Take on an empty stomach, at least 1 hour before and 2 hours after a meal.
(2.1) Swallow whole; do not cut, break or chew the tablets. (2.1) Drink an adequate amount of fluids. (2.1, 5.7) Treatment of Moderately Active Ulcerative Colitis : Recommended dosage is 1,600 mg (two 800 mg tablets) three times daily for 6 weeks.
(2.2)
2.1Important Administration Instructions Do not substitute one mesalamine delayed-release 800 mg tablet for two mesalamine delayed-release 400 mg oral products [see Clinical Pharmacology (12.3) ] . Evaluate renal function prior to initiation of mesalamine delayed-release tablets. Take mesalamine delayed-release tablets on an empty stomach, at least 1 hour before and 2 hours after a meal [see Clinical Pharmacology (12.3) ] .
Swallow mesalamine delayed-release tablets whole. Do not cut, break or chew the tablets. Drink an adequate amount of fluids [see Warnings and Precautions (5.7) ] .
Intact, partially intact, and/or tablet shells have been reported in the stool; Instruct patients to contact their healthcare provider if this occurs repeatedly. Protect mesalamine delayed-release tablets from moisture.
2.2Dosage Information For the treatment of moderately active ulcerative colitis, the recommended dosage of mesalamine delayed-release tablets in adults is 1,600 mg (two 800 mg tablets) three times daily (total daily dosage of 4.8 grams) for a duration of 6 weeks.
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Mesalamine delayed-release tablets, USP: 800 mg (red to dark red, modified oval, film-coated, biconvex, unscored tablets printed with AN360 in black ink on one side and plain on the other side). Delayed-release tablets: 800 mg (3)
⛔ Contraindications ▾
4 CONTRAINDICATIONS Mesalamine delayed-release tablets are contraindicated in patients with known or suspected hypersensitivity to salicylates or aminosalicylates or to any of the ingredients of mesalamine delayed-release tablets [see Warnings and Precautions (5.3) , Adverse Reactions (6.2) , and Description (11) ] . Known or suspected hypersensitivity to salicylates or aminosalicylates or to any of the ingredients of mesalamine delayed-release tablets (4, 5.3)
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Renal Impairment : Assess renal function at the beginning to treatment and periodically during treatment. Evaluate the risks and benefits in patients with known renal impairment or taking nephrotoxic drugs; monitor renal function. Discontinue mesalamine delayed-release if renal function deteriorates.
(5.1, 7.1, 8.6) Mesalamine-Induced Acute Intolerance Syndrome : Symptoms may be difficult to distinguish from an ulcerative colitis exacerbation; monitor for worsening symptoms; discontinue if acute intolerance syndrome suspected. (5.2) Hypersensitivity Reactions, including Myocarditis and Pericarditis : Evaluate patients immediately and discontinue if a hypersensitivity reaction is suspected. (5.3) Hepatic Failure : Evaluate the risks and benefits in patients with known liver impairment.
(5.4) Severe Cutaneous Adverse Reactions : Discontinue at the first signs or symptoms of severe cutaneous adverse reactions or other signs of hypersensitivity and consider further evaluation. (5.5) Photosensitivity : Advise patients with pre-existing skin conditions to avoid sun exposure, wear protective clothing, and use a broad-spectrum sunscreen when outdoors. (5.6) Nephrolithiasis: Mesalamine-containing stones are undetectable by standard radiography or computed tomography (CT).
Ensure adequate hydration during treatment. (5.7) Iron Content of Mesalamine Delayed-Release : Consider the iron content of mesalamine delayed-release in patients taking iron supplementation and those at risk of iron overload. (5.8) Interference with Laboratory Tests : Use of mesalamine may lead to spuriously elevated test results when measuring urinary normetanephrine by liquid chromatography with electrochemical detection.
(5.9)
5.1Renal Impairment Renal impairment, including minimal change disease, acute and chronic interstitial nephritis, and, rarely, renal failure, has been reported in patients taking products such as mesalamine delayed-release that contain or are converted to mesalamine [see Adverse Reactions (6.2) ] . In animal studies, the kidney was the principal organ of mesalamine toxicity [see Adverse Reactions (6.2) , Nonclinical Toxicology (13.2) ] . Evaluate renal function prior to initiation of mesalamine delayed-release and periodically while on therapy.
Evaluate the risks and benefits of using mesalamine delayed-release in patients with known renal impairment or history of renal disease or taking concomitant nephrotoxic drugs. Discontinue mesalamine delayed-release if renal function deteriorates while on therapy. [see Drug Interactions (7.1) , Use in Specific Populations (8.6) ] .
5.2Mesalamine-Induced Acute Intolerance Syndrome Mesalamine has been associated with an acute intolerance syndrome that may be difficult to distinguish from an exacerbation of ulcerative colitis. Exacerbation of the symptoms of colitis has been reported in 2.3% of mesalamine delayed-release-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 mesalamine delayed-release tablets as well as other mesalamine products.
Symptoms usually abate when mesalamine delayed-release tablets are discontinued. Monitor patients for worsening of these symptoms while on treatment. If acute intolerance syndrome is suspected, promptly discontinue treatment with mesalamine delayed-release.
5.3Hypersensitivity Reactions Hypersensitivity reactions have been reported in patients taking sulfasalazine. Some patients may have a similar reaction to mesalamine delayed-release tablets or to other compounds that contain or are converted to mesalamine. As with sulfasalazine, mesalamine-induced hypersensitivity reactions may present as internal organ involvement, including myocarditis, pericarditis, nephritis, hepatitis, pneumonitis, and hematologic abnormalities.
Evaluate patients…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following serious or clinically significant adverse reactions described elsewhere in labeling are: Renal Impairment [see Warnings and Precautions (5.1) ] Mesalamine-Induced Acute Intolerance Syndrome [see Warnings and Precautions (5.2) ] Hypersensitivity Reactions [see Warnings and Precautions (5.3) ] Hepatic Failure [see Warnings and Precautions (5.4) ] Severe Cutaneous Adverse Reactions [see Warnings and Precautions (5.5) ] Photosensitivity [see Warnings and Precautions (5.6) ] Nephrolithiasis [see Warnings and Precautions (5.7) ] The most common adverse reactions (≥2%) are headache, nausea, nasopharyngitis, abdominal pain, and worsening of ulcerative colitis.
(6.1) To report SUSPECTED ADVERSE REACTIONS, contact Amneal Pharmaceuticals at 1-877-835-5472 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch
6.1Clinical 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. Mesalamine delayed-release 800 mg tablets have been evaluated in 896 patients with ulcerative colitis in controlled studies. Three six-week, active-controlled studies were conducted comparing mesalamine delayed-release 800 mg tablets 4.8 grams per day with mesalamine delayed-release tablets 400 mg 2.4 grams per day in patients with mildly to moderately active ulcerative colitis.
In these studies, 727 patients were dosed with mesalamine delayed-release 800 mg tablets and 732 patients were dosed with mesalamine delayed-release 400 mg tablets. The most common reactions reported in the mesalamine delayed-release 800 mg tablet group were headache (4.7%), nausea (2.8%), nasopharyngitis (2.5%), abdominal pain (2.3%), diarrhea (1.7%), and dyspepsia (1.7%); Table 1 enumerates adverse reactions that occurred in the three studies. The most common reactions in patients with moderately active ulcerative colitis (602 patients dosed with mesalamine delayed-release 800 mg and 618 patients dosed with mesalamine delayed-release 400 mg) were the same as all treated patients.
Discontinuations due to adverse reactions occurred in 3.9% of patients in the mesalamine delayed-release 800 mg tablet group and in 4.2% of patients in the mesalamine delayed-release 400 mg tablet comparator group. The most common cause for discontinuation was gastrointestinal symptoms associated with ulcerative colitis. Serious adverse reactions occurred in 0.8% of patients in the mesalamine delayed-release 800 mg tablet group and in 1.8% of patients in the mesalamine delayed-release tablet comparator group.
The majority involved the gastrointestinal system. Table 1. Adverse Reactions Occurring in ≥1% of All Treated Patients (Three studies combined) Adverse Reaction Mesalamine delayed-release 2.4 grams per day (400 mg Tablet) (N = 732) Mesalamine delayed-release 4.8 grams per 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 % 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 Percent = percentage of patients in category and treatment group
6.2Postmarketing Experience The following adverse reactions have been identified during post-approval use of mesalamine delayed-release or other mesalamine-containing products or products that 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 fe…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Nephrotoxic Agents including NSAIDs : Increased risk of nephrotoxicity; monitor for changes in renal function and mesalamine-related adverse reactions. (7.1) Azathioprine or 6-Mercaptopurine : Increased risk of blood disorders; monitor complete blood cell counts and platelet counts. (7.2)
7.1Nephrotoxic Agents, Including Non-Steroidal Anti-Inflammatory Drugs The concurrent use of mesalamine with known nephrotoxic agents, including nonsteroidal anti-inflammatory drugs (NSAIDs) may increase the risk of nephrotoxicity. Monitor patients taking nephrotoxic drugs for changes in renal function and mesalamine-related adverse reactions [see Warnings and Precautions (5.1) ].
7.2Azathioprine or 6-Mercaptopurine The concurrent use of mesalamine with azathioprine or 6-mercaptopurine and/or other drugs known to cause myelotoxicity may increase the risk for blood disorders, bone marrow failure, and associated complications. If concomitant use of mesalamine delayed-release and azathioprine or 6-mercaptopurine cannot be avoided, monitor blood tests, including complete blood cell counts and platelet counts.
7.3Interference With Urinary Normetanephrine Measurements Use of mesalamine delayed-release may lead to spuriously elevated test results when measuring urinary normetanephrine by liquid chromatography with electrochemical detection [see Warnings and Precautions (5.9) ] . Consider an alternative, selective assay for normetanephrine.
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS Geriatric Patients : Increased risk of blood dyscrasias; monitor complete blood cell counts and platelet counts. (8.5)
8.1Pregnancy Risk Summary Limited published data on mesalamine use in pregnant women are insufficient to inform a drug-associated risk. No fetal harm was observed in animal reproduction studies of mesalamine in rats and rabbits at oral doses approximately 0.97 times (rat) and 1.95 times (rabbit) the recommended human dose (see Data ). The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown.
In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data Reproduction studies with mesalamine were performed during organogenesis in rats and rabbits at oral doses up to 480 mg/kg/day. There was no evidence of harm to the fetus.
These mesalamine doses were about 0.97 times (rat) and 1.95 times (rabbit) the recommended human dose of 4.8 grams per day, based on body surface area.
8.2Lactation Risk Summary Mesalamine and its N-acetyl metabolite are present in human milk in undetectable to small amounts ( see Data ). There are limited reports of diarrhea in breastfed infants. There is no information on the effects of the drug on milk production.
The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for mesalamine delayed-release and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition. Clinical Considerations Monitor breastfed infants for diarrhea. Data Human Data In published lactation studies, maternal mesalamine doses from various oral and rectal formulations and products ranged from 500 mg to 3 g daily.
The concentration of mesalamine in milk ranged from non-detectable to 0.11 mg/L. The concentration of the N-acetyl-5-aminosalicylic acid metabolite ranged from 5 mg/L to 18.1 mg/L. Based on these concentrations, estimated infant daily dosages for an exclusively breastfed infant are 0 mg/kg/day to 0.017 mg/kg/day of mesalamine and 0.75 mg/kg/day to 2.72 mg/kg/day of N-acetyl-5-aminosalicylic acid.
8.4Pediatric Use Safety and effectiveness of mesalamine delayed-release in pediatric patients have not been established. See the prescribing information for other approved mesalamine products for the safety and effectiveness of these products in pediatric patients.
8.5Geriatric Use Clinical studies of mesalamine delayed-release did not include sufficient numbers of patients aged 65 years and over to determine whether they respond differently than younger patients. Reports from uncontrolled clinical studies and postmarketing reporting systems suggested a higher incidence of blood dyscrasias (i.e., agranulocytosis, neutropenia, and pancytopenia) in patients who were 65 years or older compared to younger patients taking mesalamine-containing products such as mesalamine delayed-release.
Monitor complete blood cell counts and platelet counts in elderly patients during therapy with mesalamine delayed-release. In general, consider the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy in elderly patients when prescribing mesalamine delayed-release [see Use in Specific Populations (8.6) ] .
8.6Renal Impairment Mesalamine is known to be substantially excreted by the kidney, and the risk of adverse reactions may be greater in patients with impaired renal function. Evaluate renal function in all patients prior to initiation and periodically while on mesalamine delayed-release therapy. Monitor patients with known renal impairment or history of renal disease or taking nephrotoxic drugs for decreased renal function and mesalamine-related adverse reactions.
Discontinue mesalamine delayed-release if renal function deteriorates while on therapy.…
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary Limited published data on mesalamine use in pregnant women are insufficient to inform a drug-associated risk. No fetal harm was observed in animal reproduction studies of mesalamine in rats and rabbits at oral doses approximately 0.97 times (rat) and 1.95 times (rabbit) the recommended human dose (see Data ). The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown.
In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data Reproduction studies with mesalamine were performed during organogenesis in rats and rabbits at oral doses up to 480 mg/kg/day. There was no evidence of harm to the fetus.
These mesalamine doses were about 0.97 times (rat) and 1.95 times (rabbit) the recommended human dose of 4.8 grams per day, based on body surface area.
🧒 Pediatric Use ▾
8.4Pediatric Use Safety and effectiveness of mesalamine delayed-release in pediatric patients have not been established. See the prescribing information for other approved mesalamine products for the safety and effectiveness of these products in pediatric patients.
🧓 Geriatric Use ▾
8.5Geriatric Use Clinical studies of mesalamine delayed-release did not include sufficient numbers of patients aged 65 years and over to determine whether they respond differently than younger patients. Reports from uncontrolled clinical studies and postmarketing reporting systems suggested a higher incidence of blood dyscrasias (i.e., agranulocytosis, neutropenia, and pancytopenia) in patients who were 65 years or older compared to younger patients taking mesalamine-containing products such as mesalamine delayed-release.
Monitor complete blood cell counts and platelet counts in elderly patients during therapy with mesalamine delayed-release. In general, consider the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy in elderly patients when prescribing mesalamine delayed-release [see Use in Specific Populations (8.6) ] .
🆘 Overdosage ▾
10 OVERDOSAGE Mesalamine delayed-release is an aminosalicylate, and symptoms of salicylate toxicity include nausea, vomiting and abdominal pain, tachypnea, hyperpnea, tinnitus, and neurologic symptoms (headache, dizziness, confusion, seizures). Severe salicylate intoxication may lead to electrolyte and blood pH imbalance and potentially to other organ (e.g., renal and liver) involvement. There is no specific antidote for mesalamine overdose; however, conventional therapy for salicylate toxicity may be beneficial in the event of acute overdosage and may include gastrointestinal tract decontamination to prevent of further absorption.
Correct fluid and electrolyte imbalance by the administration of appropriate intravenous therapy and maintain adequate renal function. Mesalamine delayed-release tablets are a pH dependent product and this factor should be considered when treating a suspected overdose.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action The mechanism of action of mesalamine is not fully understood, but appears to be a topical anti-inflammatory effect on colonic epithelial cells. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways, that is, prostanoids, and through the lipoxygenase pathways, that is, leukotrienes and hydroxyeicosatetraenoic acids, is increased in patients with ulcerative colitis, and it is possible that mesalamine diminishes inflammation by blocking cyclooxygenase and inhibiting prostaglandin production in the colon.
12.3Pharmacokinetics Absorption Plasma concentrations of mesalamine (5-aminosalicylic acid; 5-ASA) and its metabolite, N-acetyl-5-aminosalicylic acid (N-Ac-5-ASA) are highly variable following administration of mesalamine delayed-release tablets. Following single dose oral administration of mesalamine delayed-release 800 mg tablet in healthy subjects (N = 139) under fasted conditions, the mean C max , AUC 8-48h and AUC 0-tldc values were 208 ng/mL, 2,296 ng.h/mL, and 2533 ng.h/mL, respectively. The median [range] T max for mesalamine following administration of mesalamine delayed-release 800 mg tablet was approximately 24 hours [4 hours to 72 hours], reflecting the delayed-release characteristics of the formulation.
Based on cumulative urinary recovery of mesalamine and N-Ac-5-ASA from single dose studies in healthy subjects, approximately 20% of the orally administered mesalamine in mesalamine delayed-release tablets is systemically absorbed. Food Effect: A high calorie (800 to 1,000 calories), high fat (approximately 50 % of total caloric content) meal increased mesalamine C max by 2.4-fold and mesalamine systemic exposure (AUC 8-48 and AUC 0-tldc ) by 2.8-fold; the median lag-time increased by 8 hours and median t max by 6 hours (from 24 hours to 30 hours) [see Dosage and Administration (2.1) ] .
Comparative exposure between one mesalamine delayed-release 800 mg tablet and two mesalamine delayed-release 400 mg oral products is unknown [see Dosage and Administration (2.1) ] . Elimination Metabolism The absorbed mesalamine is acetylated in the gut mucosal wall and by the liver to N-Ac-5-ASA. Excretion Absorbed mesalamine is excreted mainly by the kidneys as N-acetyl-5-aminosalicylic acid.
Unabsorbed mesalamine is excreted in feces.
🧬 Mechanism of Action ▾
12.1Mechanism of Action The mechanism of action of mesalamine is not fully understood, but appears to be a topical anti-inflammatory effect on colonic epithelial cells. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways, that is, prostanoids, and through the lipoxygenase pathways, that is, leukotrienes and hydroxyeicosatetraenoic acids, is increased in patients with ulcerative colitis, and it is possible that mesalamine diminishes inflammation by blocking cyclooxygenase and inhibiting prostaglandin production in the colon.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Mesalamine delayed-release tablets, USP 800 mg are available as red to dark red, modified oval, film-coated, biconvex, unscored tablets printed with AN360 in black ink on one side and plain on the other side. They are supplied as follows: Bottles of 180 tablets with child-resistant closure: NDC 65162-360-18 Protect from moisture. Tablets can be dispensed without desiccant for up to 6 weeks.
Store at 20° to 25° C (68° to 77° F); excursions permitted between 15° to 30° C (59° to 86° F) [see USP Controlled Room Temperature]
📋 Description ▾
11 DESCRIPTION Each mesalamine delayed-release tablet, USP for oral administration contains 800 mg of mesalamine, USP, an aminosalicylate. Mesalamine delayed-release tablets, USP have an outer protective coat consisting of a combination of acrylic based resins, methacrylic acid copolymer type A and methacrylic acid copolymer type B. The inner coat consists of an acrylic based resin, Eudragit S, which dissolves at pH 7 or greater, releasing mesalamine, USP in the terminal ileum and beyond for topical anti-inflammatory action in the colon.
Mesalamine, USP (also referred to as 5-aminosalicylic acid or 5-ASA) has the chemical name 5-amino-2-hydroxybenzoic acid; its structural formula is: Inactive Ingredients: Each tablet contains colloidal silicon dioxide, dibutyl sebacate, hypromellose, iron oxide red, iron oxide yellow, lactose monohydrate, magnesium stearate, methacrylic acid copolymer type A, methacrylic acid copolymer type B, polyethylene glycol, povidone, sodium starch glycolate, and talc. The black imprinting ink contains the following ingredients: ammonium hydroxide, iron oxide black, propylene glycol and shellac glaze.
Structural formula
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Administration [see Dosage and Administration (2.1) ] Inform patients that if they are switching from a previous oral mesalamine therapy to mesalamine delayed-release to discontinue their previous oral mesalamine therapy and follow the dosing instructions for mesalamine delayed-release. One mesalamine delayed-release 800 mg tablet is not substitutable for two mesalamine delayed-release 400 mg oral products. Inform patients to take mesalamine delayed-release tablets on an empty stomach, at least 1 hour before and 2 hours after a meal.
Instruct patients to swallow the mesalamine delayed-release tablets whole, taking care not to break, cut, or chew the tablets, because the coating is an important part of the delayed-release formulation. Drink an adequate amount of fluids. Inform patients that intact, partially intact, and/or tablet shells have been reported in the stool.
Instruct patients to contact their healthcare provider if this occurs repeatedly. Instruct patients to protect mesalamine delayed-release tablets from moisture. Renal Impairment Inform patients that mesalamine delayed-release may decrease their renal function, especially if they have known renal impairment or are taking nephrotoxic drugs, including NSAIDs, and periodic monitoring of renal function will be performed while they are on therapy.
Advise patients to complete all blood tests ordered by their healthcare provider [see Warnings and Precautions (5.1) , Drug Interactions (7.1) ] . Mesalamine-Induced Acute Intolerance Syndrome and Other Hypersensitivity Reactions Inform patients of the signs and symptoms of hypersensitivity reactions. Instruct patients to stop taking mesalamine delayed-release and report to their healthcare provider if they experience new or worsening symptoms of Acute Intolerance Syndrome (cramping, abdominal pain, bloody diarrhea, fever, headache, malaise, conjunctivitis and rash) or other symptoms suggestive of mesalamine-induced hypersensitivity [see Warnings and Precautions (5.2, 5.3) ] .
Hepatic Failure Inform patients with known liver disease of the signs and symptoms of worsening liver function and advise them to report to their healthcare provider if they experience such signs or symptoms [see Warnings and Precautions (5.4) ] . Severe Cutaneous Adverse Reactions Inform patients of the signs and symptoms of severe cutaneous adverse reactions. Instruct patients to stop taking mesalamine delayed-release and report to their healthcare provider at first appearance of a severe cutaneous adverse reaction or other sign of hypersensitivity [see Warnings and Precautions (5.5) ] .
Photosensitivity Advise patients with pre-existing skin conditions to avoid sun exposure, wear protective clothing, and use a broad-spectrum sunscreen when outdoors [see Warnings and Precautions (5.6) ] . Nephrolithiasis Instruct patients to maintain an adequate fluid intake in order to minimize the risk of kidney stone formation and to contact their healthcare provider if they experience signs or symptoms of a kidney stone (e.g., severe side or back pain, blood in the urine) [see Warnings and Precautions (5.7) ] . Iron Content of Mesalamine Delayed-Release Advise patients to inform their healthcare provider if they take iron-containing supplements [see Warnings and Precautions (5.8) ].
Blood Disorders Inform elderly patients and those taking azathioprine or 6-mercaptopurine of the risk for blood disorders and the need for periodic monitoring of complete blood cell counts and platelet counts while on therapy. Advise patients to complete all blood tests ordered by their healthcare provider [see Drug Interactions (7.2) , Use in Specific Populations (8.5) ] . Urine Discoloration Advise patients that urine may become discolored reddish-brown while taking mesalamine delayed-release tablets when it comes in contact with surfaces or water treated with hypochlorite-containing bleach.
If discolored urine is observed, advise patients to observe…