Mesalamine 500 mg Capsule, Extended Release, 120-count — NDC 63304-089-13 (Billing 63304-0089-13)
This is a package of 120 capsules of Mesalamine 500 mg Capsule, Extended Release from Sun Pharmaceutical Industries Inc., marketed since May 2022 and currently FDA-listed; retail pharmacies pay about $3.47 per capsule (NADAC). It is this product's only package size.
Identity & classification
Regulatory identifiers FDA, NLM and CMS codes for this package
Drug-database identifiers Medi-Span GPI and First Databank GCN / HICL / AHFS classification
- GSN (GCN sequence number): 058091
- GCN: 23422
- GPI-14 (Medi-Span): 52500030000220
- HICL (First Databank): 001848
- AHFS class code: 56:36.00.00
- RxCUI (RxNorm): 476362
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- FDA label on DailyMed · label index refreshed Oct 1, 2026
- RxNorm (NLM RxNav) · catalog refreshed Oct 1, 2026
- Medi-Span GPI (licensed)
- First Databank (licensed) · refreshed Oct 1, 2026
RxNorm drug class
This medicine belongs to the Aminosalicylate class.
Where does this data come from?
- RxClass (NLM) · catalog refreshed Oct 1, 2026
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 ↗- It treats ulcerative colitis and, in rectal forms, inflammation in the lower bowel such as proctitis. Some products are for flares, some for keeping remission, and some for both. Y...
- It depends on your product. Tablets and most capsules are swallowed whole. Rectal forms are usually used at bedtime. Drink plenty of fluids, and follow your label for food and timi...
- Headache, gas, belly pain and diarrhea are the common ones. Call your doctor if you get severe cramping with bloody diarrhea, fever or rash, since that could be a reaction to the d...
- Yes. Your kidney function should be checked before starting and periodically after. If you take azathioprine or 6-mercaptopurine, or are 65 or older, blood counts should be monitor...
Patient education
Supplement & herbal interactions
Some supplements/herbs that may interact with Mesalamine — tap one for details:
Where does this data come from?
- MedlinePlus (NLM) · refreshed Oct 1, 2026
- FDA label on DailyMed · label index refreshed Oct 1, 2026
Ask a licensed pharmacist directly — free, answered by our team.
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 | $3.470 | $416.45 / 120 capsules |
| Medicaid paysCMS SDUD · 12 mo | $4.40 | $528.56 / 120 capsules |
| Medicare drug plans payPart D · Q2 2026 | $4.50 | $539.57 / 120 capsules |
Where does this data come from?
- CMS NADAC weekly file · file of Jun 10, 2026
- CMS ASP pricing files · refreshed Sep 20, 2026
- CMS Medicaid State Drug Utilization Data · through Q1 2026
- CMS Part D plan pricing files · refreshed Sep 24, 2026
- VA National Acquisition Center price file
Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Marketing end | Status |
|---|---|---|---|---|
| 63304-0089-13 You're viewing this Main listing | 120 CAPSULE, EXTENDED RELEASE in 1 BOTTLE | 2022-05-13 | — | Active |
Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Mesalamine 500 mgthis 63304-0089-13 | Sun | 120 capsules | $3.470 | AB | Availability likely | — |
| Pentasa 500 mg 54092-0191-12 | Takeda | 120 capsules | $5.826 | AB | Availability likely | +68% |
| Mesalamine 500 mg 00781-2793-72 | Sandoz | 120 capsules | — | AB | FDA listed | — |
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- FDA Orange Book · refreshed Sep 3, 2026
- CMS NADAC weekly file · file of Jun 10, 2026
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?
- FDA Orange Book · refreshed Sep 3, 2026
What it looks like
Where does this data come from?
- FDA label on DailyMed · label index refreshed Oct 1, 2026
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.
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Castor oil is a natural plant-based oil used in medicines as a lubricant, laxative agent, and solvent. It helps medicine ingredients dissolve or flow smoothly and can aid bowel movement in formulations designed for that purpose.
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A food-derived fat used as an emulsifier and stabilizer. It helps blend oil and water-based ingredients together and keeps the medicine's texture consistent throughout its shelf life.
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Ethylcellulose is a plant-derived thickener and film-former made by chemically modifying cellulose. It's used as a binder to hold tablet ingredients together, a coating to control how quickly medicine is released, or a thickener in liquid formulations.
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Gelatin is a protein derived from animal collagen, commonly used in medicines as a gelling agent and capsule material. It helps create soft or hard capsule shells that hold and release medication, and can also thicken liquid formulations.
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17 inactive ingredients listed in the exact product block matched to this NDC.
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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.- FDA label on DailyMed · label index refreshed Oct 1, 2026
- FDA openFDA NDC Directory · synced Oct 1, 2026
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Manufacturer & labeler
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- Drugs@FDA
Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Mesalamine extended-release capsules are indicated for the induction of remission and for the treatment of mildly to moderately active ulcerative colitis in adult patients. Mesalamine extended-release capsules are an aminosalicylate indicated for the induction of remission and for the treatment of mildly to moderately active ulcerative colitis in adult patients. (1)
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Evaluate renal function prior to initiation of mesalamine extended-release capsules and periodically while on therapy [see Warnings and Precautions (5.1)] . Recommended Dosage The recommended dosage for the induction of remission and the symptomatic treatment of mildly to moderately active ulcerative colitis in adults is 1 g (2 mesalamine extended-release 500 mg capsules) administered orally four times daily. Administration Instructions Swallow mesalamine extended-release capsules whole; do not crush or chew.
Alternatively, the capsule(s) may be opened and the entire contents sprinkled onto applesauce or yogurt. Consume the entire mixture immediately. Drink an adequate amount of fluids during treatment [see Warnings and Precautions (5.7)] .
Evaluate renal function prior to initiation of mesalamine extended-release capsules and periodically while on therapy. (2, 5.1) The recommended dosage is 1 g administered orally four times daily. (2) Swallow capsules whole; do not crush or chew.
(2) Alternatively, the capsule(s) may be opened and the contents sprinkled onto applesauce or yogurt. (2) Drink an adequate amount of fluids. (2, 5.7)
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Extended-release capsule 500 mg are hard gelatin having dark blue cap and body with “ RL36 ” printed on both cap and body in black ink containing off-white to light yellowish brown to dark yellowish brown colored pellets. Extended-release capsule: 500 mg. (3)
⛔ Contraindications ▾
4 CONTRAINDICATIONS Mesalamine extended-release capsules are contraindicated in patients with known or suspected hypersensitivity to salicylates, aminosalicylates, or any ingredients of mesalamine extended-release capsules [see Warnings and Precautions (5.3)] . Known or suspected hypersensitivity to salicylates or aminosalicylates or to any of the ingredients of mesalamine extended-release capsules. (4, 5.3)
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS • Renal Impairment: Assess renal function at the beginning of treatment and periodically during treatment. Evaluate the risks and benefits of mesalamine in patients with known renal impairment or taking nephrotoxic drug. Discontinue mesalamine if renal function deteriorates while on therapy.
(5.1, 7.1, 8.6) • Mesalamine-Induced Acute Intolerance Syndrome: Discontinue treatment if acute intolerance syndrome (cramping, acute abdominal pain, bloody diarrhea, sometimes fever, headache and rash) is suspected. (5.2) Hypersensitivity Reactions, including myocarditis and pericarditis : Discontinue mesalamine if a hypersensitivity reaction is suspected. (5.3) Hepatic Failure: Evaluate the risks and benefits of using mesalamine 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 : Avoid sun exposure if pre-existing skin conditions. (5.6) Nephrolithiasis: Cases of nephrolithiasis have been reported with the use of mesalamine.
Mesalamine-containing stones are undetectable by standard radiography or computed tomography (CT). Ensure adequate hydration during treatment. (5.7) Interference with Laboratory Tests: Mesalamine may lead to elevated urinary normetanephrine test results.
(5.8)
5.1Renal Impairment Renal impairment, including minimal change disease, acute and chronic interstitial nephritis, and renal failure have been reported in patients given mesalamine or other products that contain mesalamine or are converted to mesalamine. Evaluate the risks and benefits of using mesalamine in patients with known renal impairment or a history of renal disease or taking concomitant nephrotoxic drugs. Evaluate renal function in all patients prior to initiation and periodically while on therapy with mesalamine.
Discontinue mesalamine 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. Symptoms include cramping, acute abdominal pain, bloody diarrhea, and sometimes fever, headache, and rash. Monitor patients for worsening of these symptoms while on treatment.
If acute intolerance syndrome is suspected, promptly discontinue treatment with mesalamine.
5.3Hypersensitivity Reactions Hypersensitivity reactions have been reported in patients taking sulfasalazine. Some patients may have a similar reaction to mesalamine 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 immediately if signs or symptoms of a hypersensitivity reaction are present. Discontinue mesalamine if an alternative etiology for the signs and symptoms cannot be established.
5.4Hepatic Failure There have been reports of hepatic failure in patients with pre-existing liver disease who have been administered other products containing mesalamine. Evaluate the risks and benefits of using mesalamine in patients with known liver impairment.
5.5Severe Cutaneous Adverse Reactions Severe cutaneous adverse reactions, such as Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN), drug reaction with eosinophilia and systemic symptoms (DRESS), and acute generalized exanthematous pustulosis (AGEP) have been reported in with the use of mesalamine [see Adverse Reactions (6.2)] . Discontinue mesalamine at the first signs or symptoms of severe cutaneous adverse reactions or other signs of hypersensitivity and consider further evaluation
5.6Photosensitivity Patients… [Excerpted — this section continues on DailyMed.]
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: 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)] Most common adverse reactions are nausea and vomiting (1%).
(6.1) To report SUSPECTED ADVERSE REACTIONS, contact Sun Pharmaceutical Industries, Inc. at 1-800-818-4555 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. More than 2,100 patients were exposed to mesalamine in clinical trials of ulcerative colitis or another gastrointestinal condition. The most common adverse reactions (i.e., greater than or equal to 1%) were diarrhea (3%), headache (2%), nausea (2%), abdominal pain (2%), dyspepsia (2%), vomiting (2%), and rash (1%).
The safety of mesalamine was evaluated in two randomized, double-blind, placebo-controlled, dose-response trials (UC-1 and UC-2) of 624 patients with mildly to moderately active ulcerative colitis for up to 8 weeks of treatment [see Clinical Studies (14)] . The most common adverse reaction was nausea and vomiting: 1% in the mesalamine group (N = 451) and 0% in the placebo group (N = 173). Withdrawal from therapy due to adverse reactions was 7% in the mesalamine group and 4% in the placebo group.
The following adverse reactions, presented by body system, were reported in less than 1% of patients in UC-1, UC-2, and clinical trials for another gastrointestinal condition. Blood and lymphatic system disorders: thrombocythemia, thrombocytopenia Cardiac Disorders: palpitations, pericarditis, vasodilation Gastrointestinal Disorders: abdominal distention, constipation, duodenal ulcer, dysphagia, eructation, esophageal ulcer, fecal incontinence, GI bleeding, mouth ulcer, pancreatitis, rectal bleeding, stool abnormalities (color or texture change) General disorders and administration site conditions: fever, malaise Infections and infestations: oral moniliasis, conjunctivitis Investigations: GGTP increase, increased alkaline phosphatase, LDH increase, SGOT increase, SGPT increase, lipase increase, amylase increase Metabolism and nutritional disorders: anorexia, edema, thirst Musculoskeletal and connective tissue disorders: arthralgia, leg cramps, myalgia Nervous System Disorders: dizziness, insomnia, somnolence, paresthesia Psychiatric disorders: depression, asthenia Renal and urinary disorders: albuminuria, hematuria, urinary frequency Reproductive system and breast disorders: amenorrhea, breast pain, hypomenorrhea, menorrhagia, metrorrhagia Respiratory, Thoracic and Mediastinal Disorders: pulmonary infiltrates, one week after completion of an 8-week ulcerative colitis study, a 72-year-old male, with no previous history of pulmonary problems, developed dyspnea.
The patient was subsequently diagnosed with interstitial pulmonary fibrosis without eosinophilia by one physician and bronchiolitis obliterans with organizing pneumonitis by a second physician. Skin and Subcutaneous Tissue Disorders: acne, alopecia, dry skin, eczema, erythema nodosum, nail disorder, photosensitivity, pruritus, sweating, urticaria, ecchymosis, lichen planus
6.2Postmarketing Experience The following adverse reactions have been identified during post-approval use of mesalamine. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their… [Excerpted — this section continues on DailyMed.]
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Nephrotoxic Agents including Non-Steroidal Anti-inflammatory Drugs (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 dyscrasias; 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 non-steroidal 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 any other drugs known to cause myelotoxicity may increase the risk for blood disorders, bone marrow failure, and associated complications. If concomitant use of mesalamine 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 may lead to spuriously elevated test results when measuring urinary normetanephrine by liquid chromatography with electrochemical detection [see Warnings and Precautions (5.8)] . 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 Published data from meta-analyses, cohort studies, and case series on the use of mesalamine during pregnancy have not reliably informed an association with mesalamine and major birth defects, miscarriage, or adverse maternal or fetal outcomes (see Data) . There are adverse effects on maternal and fetal outcomes associated with ulcerative colitis in pregnancy (see Clinical Considerations). In animal reproduction studies, oral administration of mesalamine during organogenesis to pregnant rats at doses up to 1000 mg/kg/day (approximately 2.4 times the maximum recommended human dose of 4 g/day, based on a body surface area comparison) and rabbits at doses of 800 mg/kg/day (approximately 3.9 times the maximum recommended human dose of 4 g/day, based on a body surface area comparison) revealed no evidence of adverse developmental effects (see Data) .
The background risk of major birth defects and miscarriage for the indicated populations is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriages in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.
Clinical Considerations Disease-associated maternal and embryo/fetal risk Published data suggest that increased disease activity is associated with the risk of developing adverse pregnancy outcomes in women with ulcerative colitis. Adverse pregnancy outcomes include preterm delivery (before 37 weeks of gestation), low birth weight (less than 2500 g) infants, and small for gestational age at birth. Data Human Data Published data from meta-analyses, cohort studies, and case series on the use of mesalamine during early pregnancy (first trimester) and throughout pregnancy have not reliably informed an association of mesalamine and major birth defects, miscarriage, or adverse maternal or fetal outcomes.
There is no clear evidence that mesalamine exposure in early pregnancy is associated with an increased risk of major congenital malformations, including cardiac malformations. Published epidemiologic studies have important methodological limitations which hinder interpretation of the data, including inability to control for confounders, such as underlying maternal disease, maternal use of concomitant medications, and missing information on the dose and duration of use for mesalamine products. Animal Data Reproduction studies with mesalamine during organogenesis have been performed in pregnant rats at doses up to 1000 mg/kg/day (approximately 2.4 times the maximum recommended human dose of 4 g/day, based on a body surface area comparison) and rabbits at doses up to 800 mg/kg/day (approximately 3.9 times the maximum recommended human dose of 4 g/day based on a body surface area comparison) and have revealed no evidence of harm to the fetus due to mesalamine.
8.2Lactation Risk Summary Data from published literature report the presence of mesalamine and its metabolite, N-acetyl-5-aminosalicylic acid in human milk in small amounts with relative infant doses (RID) of 0.1% or less for mesalamine (see Data) . There are case reports of diarrhea observed in breastfed infants exposed to mesalamine (see Clinical Considerations) . There is no information on the effects of mesalamine on milk production.
The lack of clinical data during lactation precludes a clear determination of the risk of mesalamine to an infant during lactation; therefore, the developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for mesalamine and any potential adverse effects on the breastfed child from mesalamine or from the underlying maternal condition. Clinical Considerations Advise the caregiver to monitor the breastfed infant for diarr… [Excerpted — this section continues on DailyMed.]
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary Published data from meta-analyses, cohort studies, and case series on the use of mesalamine during pregnancy have not reliably informed an association with mesalamine and major birth defects, miscarriage, or adverse maternal or fetal outcomes (see Data) . There are adverse effects on maternal and fetal outcomes associated with ulcerative colitis in pregnancy (see Clinical Considerations). In animal reproduction studies, oral administration of mesalamine during organogenesis to pregnant rats at doses up to 1000 mg/kg/day (approximately 2.4 times the maximum recommended human dose of 4 g/day, based on a body surface area comparison) and rabbits at doses of 800 mg/kg/day (approximately 3.9 times the maximum recommended human dose of 4 g/day, based on a body surface area comparison) revealed no evidence of adverse developmental effects (see Data) .
The background risk of major birth defects and miscarriage for the indicated populations is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriages in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.
Clinical Considerations Disease-associated maternal and embryo/fetal risk Published data suggest that increased disease activity is associated with the risk of developing adverse pregnancy outcomes in women with ulcerative colitis. Adverse pregnancy outcomes include preterm delivery (before 37 weeks of gestation), low birth weight (less than 2500 g) infants, and small for gestational age at birth. Data Human Data Published data from meta-analyses, cohort studies, and case series on the use of mesalamine during early pregnancy (first trimester) and throughout pregnancy have not reliably informed an association of mesalamine and major birth defects, miscarriage, or adverse maternal or fetal outcomes.
There is no clear evidence that mesalamine exposure in early pregnancy is associated with an increased risk of major congenital malformations, including cardiac malformations. Published epidemiologic studies have important methodological limitations which hinder interpretation of the data, including inability to control for confounders, such as underlying maternal disease, maternal use of concomitant medications, and missing information on the dose and duration of use for mesalamine products. Animal Data Reproduction studies with mesalamine during organogenesis have been performed in pregnant rats at doses up to 1000 mg/kg/day (approximately 2.4 times the maximum recommended human dose of 4 g/day, based on a body surface area comparison) and rabbits at doses up to 800 mg/kg/day (approximately 3.9 times the maximum recommended human dose of 4 g/day based on a body surface area comparison) and have revealed no evidence of harm to the fetus due to mesalamine.
🧒 Pediatric Use ▾
8.4Pediatric Use Safety and effectiveness in pediatric patients have not been established.
🧓 Geriatric Use ▾
8.5Geriatric Use Clinical trials of mesalamine did not include sufficient numbers of patients aged 65 years and over to determine whether they respond differently from 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 receiving mesalamine-containing products such as mesalamine who were 65 years or older compared to younger adult patients, which may also be associated with ulcerative colitis, use of interacting drugs, or reduced renal function.
Monitor complete blood cell counts and platelet counts in patients 65 years and over during treatment with mesalamine. In general, consider the greater frequency of decreased hepatic, renal, or cardiac function, and of concurrent disease or other drug therapy in patients 65 years and over when prescribing mesalamine.
🆘 Overdosage ▾
10 OVERDOSAGE Mesalamine is an aminosalicylate, and symptoms of salicylate toxicity may be possible, such as: nausea, vomiting, abdominal pain, tachypnea, hyperpnea, tinnitus, and neurologic symptoms (headache, dizziness, confusion, seizures). Severe intoxication with salicylates may lead to electrolyte and blood pH imbalance and potentially to other organ (e.g., renal and liver) damage. 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 further absorption.
Correct fluid and electrolyte imbalance by the administration of appropriate intravenous therapy and maintain adequate renal function.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action The mechanism of action of mesalamine is not fully understood, but it appears to be a topical anti- inflammatory effect on colonic epithelial cells. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways (i.e., prostanoids) and through the lipoxygenase pathways (i.e., 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.
12.2Pharmacodynamics The exposure-response relationship and time course of pharmacodynamic response for the safety and effectiveness of mesalamine have not been fully characterized.
12.3Pharmacokinetics Absorption Following oral administration 20% to 30% of the mesalamine in mesalamine extended-release capsules is absorbed based on urinary excretion data. Plasma mesalamine concentration peaked at approximately 1 mcg/mL 3 hours following a 1 g mesalamine extended-release capsules dose. Oral mesalamine pharmacokinetics were nonlinear when mesalamine extended-release capsules were dosed from 250 mg to 1 g four times daily, with steady-state mesalamine plasma concentrations increasing about nine times, from 0.14 mcg/mL to 1.21 mcg/mL.
The major metabolite of mesalamine (5-aminosalicylic acid), N-acetyl-5-aminosalicylic acid, peaked at approximately 3 hours at 1.8 mcg/mL. N-acetyl-5-aminosalicylic acid pharmacokinetics were linear. Distribution Mesalamine is approximately 43% bound to plasma proteins at the concentration of 2.5 mcg/mL.
Elimination Metabolism The greater than dose proportional increase in PK of mesalamine suggests saturable first pass metabolism. The major metabolite of mesalamine, N-acetyl-5-aminosalicylic acid, is formed due to action of N-acetyltransferase in the liver and intestinal mucosa. Pharmacological activities of N-acetyl-5-aminosalicylic acid are unknown, and other metabolites have not been identified.
Excretion Following oral administration, plasma mesalamine concentration declined in a biphasic manner after reaching peak concentration. The literature describes a mean terminal half-life of 42 minutes for mesalamine following intravenous administration. Because of the continuous release and absorption of mesalamine from mesalamine extended-release capsules throughout the gastrointestinal tract, the true elimination half-life cannot be determined after oral administration.
N-acetyl-5-aminosalicylic acid was the primary compound excreted in the urine (19% to 30%) following mesalamine extended-release capsules dosing. About 130 mg free mesalamine was recovered in the feces following a single 1g mesalamine extended-release capsules dose. Elimination of free mesalamine and salicylates in feces increased proportionately with mesalamine extended-release capsules dose.
🧬 Mechanism of Action ▾
12.1Mechanism of Action The mechanism of action of mesalamine is not fully understood, but it appears to be a topical anti- inflammatory effect on colonic epithelial cells. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways (i.e., prostanoids) and through the lipoxygenase pathways (i.e., 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 extended-release capsules, USP are supplied as shown in the table: Strength Description Supplied As NDC Number 500 mg extended-release capsules, USP are hard gelatin having dark blue cap and body with “ RL36 ” printed on both cap and body in black ink containing off-white to light yellowish brown to dark yellowish brown colored pellets. bottles of 120 capsules NDC 63304-089-13 (with child-resistant closure) Store at 20 ° C to 25 ° C (68 ° F to 77 ° F). [See USP Controlled Room Temperature].
Preserve in tight, light-resistant containers.
📋 Description ▾
11 DESCRIPTION Mesalamine extended-release capsules, USP for oral administration are an extended-release formulation of mesalamine, USP, an aminosalicylate anti-inflammatory agent for gastrointestinal use. Mesalamine, USP (also referred to as 5-aminosalicylic acid or 5-ASA) has the chemical name benzoic acid, 5-amino-2-hydroxy. It has a molecular weight of 153.14.
The structural formula is: Each 500 mg mesalamine extended-release capsule, USP contains 500 mg of mesalamine, USP. It also contains the following inactive ingredients: castor oil, colloidal silicon dioxide, diacetylated monoglyceride, ethylcellulose, hypromellose, stearic acid, sugar spheres (corn starch and sucrose), talc, and white wax. The capsule shell contains FD&C Blue 1, gelatin, sodium lauryl sulfate, and titanium dioxide.
The imprinting ink contains ferrosoferric oxide, potassium hydroxide, and shellac. Meets USP dissolution Test 4. image description
🔬 Clinical Studies ▾
14 CLINICAL STUDIES In two randomized, double-blind, placebo-controlled, dose-response trials (UC-1 and UC-2) of 625 patients with active mild to moderate ulcerative colitis, mesalamine, at an oral dose of 1 g administered four times a day for up to 8 weeks, produced consistent improvement in prospectively identified primary efficacy parameters, Physical Global Assessment, Treatment Failure, and Sigmoidoscopic Index as shown in Table 2 . A mesalamine dosage regimen of 1 g four times a day demonstrated consistent improvement in secondary efficacy parameters, namely the frequency of trips to the toilet, stool consistency, rectal bleeding, abdominal/rectal pain, and urgency.
A mesalamine dosage regimen of 1 g four times a day also induced remission as assessed by endoscopic and symptomatic endpoints. Table 2: Efficacy Parameters in Adults Patients with Mildly to Moderately Active Ulcerative Colitis in Placebo-Controlled, Dose-Response Trials (UC-1 and UC-2) Parameter Clinical Trial UC-1 Clinical Trial UC-2 Evaluated Placebo N = 90 Mesalamine 1 g four times a day N = 95 Placebo N = 83 Mesalamine 1 g four times a day N = 85 Physician Global Assessment 1 36% 59%* 31% 55%* Treatment Failure 2 22% 9%* 31% 9%* Sigmoidoscopic Index 3 -2.5 -5.0* -1.6 -3.8* Remission 4 12% 26%* 12% 27%* * p< 0.05 vs placebo.
1 proportion of patients with complete or marked improvement. 2 proportion of patients developing severe or fulminant UC requiring steroid therapy or hospitalization or worsening of the disease at 7 days of therapy, or lack of significant improvement by 14 days of therapy. 3 an objective measure of disease activity rated by a standard (15-point) scale that includes mucosal vascular pattern, erythema, friability, granularity/ulcerations, and mucopus: improvement over baseline.
4 defined as complete resolution of symptoms plus improvement of endoscopic endpoints. To be considered in remission, patients had a “1” score for one of the endoscopic components (mucosal vascular pattern, erythema, granularity, or friability) and “0” for the others.
🧪 Nonclinical Toxicology ▾
13 NONCLINICAL TOXICOLOGY
13.1Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenesis In a 104-week dietary carcinogenicity study of mesalamine, CD-1 mice were administered doses up to 2500 mg/kg/day and it was not tumorigenic. The 2500 mg/kg/day dose represents approximately 2.5 times the maximum recommended human dose on a body surface area basis. In a 104-week dietary carcinogenicity study in Wistar rats, mesalamine up to a dose of 800 mg/kg/day was not tumorigenic.
This dose represents approximately 1.5 times the maximum recommended human dose on a body surface area basis. Mutagenesis No evidence of mutagenicity was observed in an in vitro Ames test and in an in vivo mouse micronucleus test. Impairment of Fertility No effects on fertility or reproductive performance were observed in male or female rats at oral doses of mesalamine up to 400 mg/kg/day (0.8 times the maximum recommended human dose based on body surface area).
📄 Package Label / Principal Display Panel ▾
Package/Label Display Panel NDC 63304-089-13 Mesalamine Extended-Release Capsules, USP 500 mg Rx only 120 Capsules SUN PHARMA image description