Mesalamine 1000 mg Suppository, 72 suppositories
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
Rectal mesalamine is used to treat ulcerative colitis (a condition which causes swelling and sores in the lining of the colon [large intestine] and rectum), proctitis (swelling in the rectum), and proctosigmoiditis (swelling in the rectum and sigmoid colon [last section of the colon]). Rectal 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?
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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.
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UNII 8334LX7S21
A solid fat derived from animal or vegetable sources, used as a coating agent and lubricant to help pills slide smoothly during manufacturing and protect the medicine from moisture and air.
1 inactive ingredient 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.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 each | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · Q2 2026 | $3.04 | $218.89 / 72 suppositories |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Mesalamine 1000 mg 00472-1915-30 | Actavis | 30 suppositories | $1.287 | AB | Availability likely | — |
| Mesalamine 1000 mg 16714-0245-30 | Northstar | 30 suppositories | $1.287 | AB | Availability likely | — |
| Mesalamine 1000 mg 31722-0005-30 | Camber | 30 suppositories | $1.287 | AB | Availability likely | — |
| Mesalamine 1000 mg 64980-0282-03 | Rising | 30 suppositories | $1.287 | AB | Availability likely | — |
| Mesalamine Rectal 1000 mg 69918-0560-30 | Amring | 30 suppositories | $1.287 | AB | Availability likely | — |
| Mesalamine 1000 mg 70710-1302-07 | Zydus | 30 suppositories | $1.287 | AB | Availability likely | — |
| Mesalamine 1000 mgthis 16571-0246-72 | Rising | 72 suppositories | — | AB | FDA listed | — |
| Canasa 1000 mg 58914-0501-33 | Allergan, | 3 suppositories | — | AB | FDA listed | — |
| Mesalamine 1000 mg 63629-2397-01 | Bryant | 30 suppositories | — | AB | FDA listed | — |
| Mesalamine 1000 mg 70771-1513-07 | Zydus | 30 suppositories | — | AB | FDA listed | — |
| Mesalamine 1000 mg 72162-1804-01 | Bryant | 30 suppositories | — | AB | FDA listed | — |
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⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
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💊 Medicaid utilization by pack size
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
📦 Packaging — all sizes for this product
| Package NDC | Description | Per unit | Per pack | Marketing start | Status |
|---|---|---|---|---|---|
| 16571-0246-03 | 5 BLISTER PACK in 1 CARTON (16571-246-03) / 6 SUPPOSITORY in 1 BLISTER PACK (16571-246-16) | $1.29 / ea | $38.60 | 2025-04-14 | Active |
| 16571-0246-72 You're viewing this | 12 BLISTER PACK in 1 CARTON (16571-246-72) / 6 SUPPOSITORY in 1 BLISTER PACK (16571-246-16) | — | — | 2025-04-14 | Active |
This pack shows little to no recent Medicaid volume — a different pack size carries most fills. See all packs ↓
Pack size FAQ
What quantity is in NDC 16571-0246-72?
What is the difference between NDC 16571-0246-72 and NDC 16571-0246-03?
What NDC number is used to bill for this package of Mesalamine 1000 mg Suppository?
Prices are the latest CMS NADAC pharmacy acquisition cost per NDC; per-pack figures are per-unit × pack quantity, shown only when the pack is denominated in the same measure NADAC prices.
🧭 About this NDC listing & data coverage
What data is (and isn’t) available for this NDC — tap to expand
| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold. |
Questions about this listing
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Mesalamine suppositories are indicated in adults for the treatment of mildly to moderately active ulcerative proctitis. Mesalamine suppositories are an aminosalicylate indicated in adults for the treatment of mildly to moderately active ulcerative proctitis. (1)
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Dosage The recommended dosage of mesalamine suppositories in adults is 1,000 mg administered rectally once daily at bedtime for 3 to 6 weeks depending on symptoms and sigmoidoscopic findings. Safety and effectiveness of mesalamine suppositories beyond 6 weeks have not been established. Administration Instructions: • Evaluate renal function prior to initiation of mesalamine suppository therapy [see Warnings and Precautions ( 5.1 )]. • Do not cut or break the suppository. • Retain the suppository for one to three hours or longer, if possible. • Drink an adequate amount of fluids [see Warnings and Precautions ( 5.7 )] • If a dose of mesalamine suppository is missed, administer as soon as possible, unless it is almost time for next dose.
Do not use two mesalamine suppositories at the same time to make up for a missed dose. • Mesalamine suppositories will cause staining of direct contact surfaces, including but not limited to fabrics, flooring, painted surfaces, marble, granite, vinyl, and enamel. Keep mesalamine suppositories away from these surfaces to prevent staining. Dosage The recommended adult dosage is 1,000 mg administered rectally once daily at bedtime for 3 to 6 weeks.
Safety and effectiveness beyond 6 weeks have not been established. ( 2 ) Administration Instructions: • Evaluate renal function prior to initiation of mesalamine suppositories and periodically while on therapy. ( 2 , 5.1 ) • Do not cut or break the suppository.
( 2 ) • Drink an adequate amount of fluids. ( 2 , 5.7 ) • Retain the suppository for one to three hours or longer, if possible. ( 2 ) • Mesalamine suppositories will cause staining of direct contact surfaces, including but not limited to fabrics, flooring, painted surfaces, marble, granite, vinyl, and enamel.
Keep mesalamine suppositories away from these surfaces to prevent staining. ( 2 )
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Mesalamine Suppository, USP: 1,000 mg mesalamine in an off white to light brown opaque bullet shaped suppository. Suppository: 1,000 mg ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS Mesalamine is contraindicated in patients with known or suspected hypersensitivity to salicylates or aminosalicylates or to any ingredients in the suppository vehicle [see Warnings and Precautions ( 5.3 ), Adverse Reactions ( 6.2 ), and Description ( 11 )]. Known or suspected hypersensitivity to salicylates or aminosalicylates or to any ingredients in the formulation. ( 4 , 5.3 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS • Renal Impairment: Evaluate the risks and benefits in patients with known renal impairment or taking nephrotoxic drugs; monitor renal function. Discontinue mesalamine suppositories if renal function deteriorates. ( 5.1 , 7.1 , 8.6 ) • Mesalamine-Induced Acute Intolerance Syndrome: Symptoms may be difficult to distinguish from an exacerbation of ulcerative colitis; monitor for worsening symptoms; discontinue treatment if acute intolerance syndrome is 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 ) • Interaction with Laboratory Test for Urinary Normetanephrine: Spuriously elevated test results may occur with liquid chromatography with electrochemical detection in patients receiving mesalamine; use alternative, selective assay for normetanephrine. ( 5.8 )
5.1Renal Impairment Renal impairment, including minimal change disease, acute and chronic interstitial nephritis, and renal failure, has been reported in patients given products such as mesalamine suppositories that contain mesalamine or are converted to mesalamine. 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 and periodically while on therapy.
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. Discontinue mesalamine suppositories 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. Although the exact frequency of occurrence has not been determined, it has occurred in 3% of patients in controlled clinical trials of mesalamine or sulfasalazine. Symptoms include cramping, acute abdominal pain and bloody diarrhea, and sometimes fever, headache, malaise, pruritus, conjunctivitis, 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 suppositories 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 suppositories 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.…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following serious or clinically significant adverse reactions are described elsewhere in 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 )] The most common adverse reactions (≥ 1%) are: dizziness, rectal pain, fever, rash, acne and colitis.
( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Rising Pharma Holdings, Inc. at 1-844-874-7464 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. The most common adverse reactions in adult patients with mildly to moderately active ulcerative proctitis in double-blind, placebo-controlled trials are summarized in the Table 1 below. Table 1: Adverse Reactions Occurring in More Than 1% of Mesalamine Suppository Treated Patients (Comparison to Placebo) Symptom Mesalamine (n=177) Placebo (n=84) N % N % Dizziness 5 3 2
2.4Rectal Pain 3 1.8 0 0 Fever 2 1.2 0 0 Rash 2 1.2 0 0 Acne 2 1.2 0 0 Colitis 2 1.2 0 0 In a multicenter, open-label, randomized, parallel group study in 99 patients comparing the mesalamine 1,000 mg suppository administered nightly to that of the mesalamine 500 mg suppository twice daily. The most common adverse reactions in both groups were headache (14%), flatulence (5%), abdominal pain (5%), diarrhea (3%), and nausea (3%). Three (3) patients discontinued medication because of an adverse reaction; one of these adverse reactions (headache) was deemed possibly related to study medication.
The recommended dosage of mesalamine suppository is 1,000 mg administered rectally once daily at bedtime [ see Dosage and Administration ( 2 )].
6.2Postmarketing Experience The following adverse reactions have been identified during post-approval use of mesalamine suppositories or other mesalamine-containing products. 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: drug fever, fatigue, lupus-like syndrome, medication residue • Cardiac Disorders: myocarditis, pericarditis, pericardial effusion [see Warnings and Precautions ( 5.3 )] • Endocrine: Nephrogenic diabetes insipidus • Eye disorders: eye swelling • Gastrointestinal Disorders: abdominal cramps, abdominal distension, anal pruritus, anorectal discomfort, constipation, feces discolored, flatulence, frequent bowel movements, gastrointestinal bleeding, mucus stools, nausea, painful defecation, pancreatitis, proctalgia, rectal discharge, rectal tenesmus, stomach discomfort, vomiting • Hepatic Disorders: cholestatic jaundice, hepatitis, jaundice, Kawasaki-like syndrome including changes in liver enzymes, liver necrosis, liver failure • Hematologic Disorders: agranulocytosis, aplastic anemia, thrombocytopenia • Neurological/Psychiatric Disorders: Guillain-Barre syndrome, peripheral neuropathy, transverse myelitis, intracranial hypertension • Renal Disorders: interstitial nephritis, renal failure, minimal change disease, nephrolithiasis [see Warnings and Precautions ( 5.1 , 5.7 )] o Urine discoloration occurring ex-vivo caused by contact of mesalamine, including inactive metabolite, with surfaces or water treated with hypochlorite containing bleach • Respiratory, Thoracic and Mediastinal Disorders: hypersensitivity pneumonitis (including allergic…
🔄 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 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, because of the similarity in the chromatograms of normetanephrine and mesalamine's main metabolite, N-acetylaminosalicylic acid. Consider an alternative, selective assay for normetanephrine [see Warnings and Precautions ( 5.8 )].
👥 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 evidence of teratogenicity was observed in rats or rabbits when treated during gestation with orally administered mesalamine at doses greater than the recommended human intra-rectal dose (see Data). The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown.
Adverse outcomes in pregnancy occur regardless of the health of the mother or the use of medications. 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 have been performed in rats at oral doses up to 320 mg/kg/day (about 1.7 times the recommended human intra-rectal dose of mesalamine, based on body surface area) and in rabbits at oral doses up to 495 mg/kg/day (about 5.4 times the recommended human intra-rectal dose of mesalamine, based on body surface area) following administration during the period of organogenesis, and have revealed no evidence of impaired fertility or harm to the fetus due to mesalamine.
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 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 conditions. Clinical Considerations Monitor breastfed infants for diarrhea. 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 to 18.1 mg/L. Based on these concentrations, estimated infant daily dosages for an exclusively breastfed infant are 0 to 0.017 mg/kg/day of mesalamine and 0.75 to 2.72 mg/kg/day of N-acetyl-5-aminosalicylic acid.
8.4Pediatric Use The safety and effectiveness of mesalamine in pediatric patients for the treatment of mildly to moderately active ulcerative proctitis have not been established. Mesalamine suppositories were evaluated for the treatment of ulcerative proctitis in a 6-week, open-label, single-arm study in 49 patients 5 to 17 years of age, which only included 14 patients with histologically-confirmed cases of ulcerative proctitis. However, efficacy was not demonstrated.
Adverse reactions seen in pediatric patients in this trial (abdominal pain, headache, pyrexia, pharyngolaryngeal pain, diarrhea and vomiting) were similar to those seen in adult patients.
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 suppositories who were 65 years or older compared to younger patients. Monitor complete blood cell counts and platelet counts in elderly patients during treatment with mesalamine suppositories.
In general, consider the greater frequency of decreased hepatic, renal,…
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary Limited published data on mesalamine use in pregnant women are insufficient to inform a drug-associated risk. No evidence of teratogenicity was observed in rats or rabbits when treated during gestation with orally administered mesalamine at doses greater than the recommended human intra-rectal dose (see Data). The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown.
Adverse outcomes in pregnancy occur regardless of the health of the mother or the use of medications. 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 have been performed in rats at oral doses up to 320 mg/kg/day (about 1.7 times the recommended human intra-rectal dose of mesalamine, based on body surface area) and in rabbits at oral doses up to 495 mg/kg/day (about 5.4 times the recommended human intra-rectal dose of mesalamine, based on body surface area) following administration during the period of organogenesis, and have revealed no evidence of impaired fertility or harm to the fetus due to mesalamine.
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and effectiveness of mesalamine in pediatric patients for the treatment of mildly to moderately active ulcerative proctitis have not been established. Mesalamine suppositories were evaluated for the treatment of ulcerative proctitis in a 6-week, open-label, single-arm study in 49 patients 5 to 17 years of age, which only included 14 patients with histologically-confirmed cases of ulcerative proctitis. However, efficacy was not demonstrated.
Adverse reactions seen in pediatric patients in this trial (abdominal pain, headache, pyrexia, pharyngolaryngeal pain, diarrhea and vomiting) were similar to those seen in adult patients.
🧓 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 suppositories who were 65 years or older compared to younger patients. Monitor complete blood cell counts and platelet counts in elderly patients during treatment with mesalamine suppositories.
In general, consider the greater frequency of decreased hepatic, renal, or cardiac function, and of concurrent disease or other drug therapy in elderly patients when prescribing mesalamine suppositories [see Use in Specific Populations ( 8.6 )].
🆘 Overdosage ▾
10 OVERDOSAGE Mesalamine absorption from the colon is limited; however, mesalamine 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.
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 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.
12.3Pharmacokinetics Absorption Mesalamine (5-ASA) administered as a rectal suppository is variably absorbed. In patients with ulcerative colitis treated with mesalamine 500 mg rectal suppositories, administered once every eight hours for six days, the mean mesalamine peak plasma concentration (C max ) was 353 ng/mL (CV=55%) following the initial dose and 361 ng/mL (CV=67%) at steady state. The mean minimum steady state plasma concentration (C min ) was 89 ng/mL (CV=89%).
Absorbed mesalamine does not accumulate in the plasma. Distribution Mesalamine administered as a rectal suppository distributes in rectal tissue to some extent. Elimination In patients with ulcerative proctitis treated with mesalamine 500 mg as a rectal suppository every 8 hours for 6 days, the mean elimination half-life was 5 hours (CV=73%) for 5-ASA and 5 hours (CV=63%) for N-acetyl-5-ASA, the active metabolite, following the initial dose.
At steady state, the mean elimination half-life was 7 hours for both 5-ASA and N-acetyl-5-ASA (CV=102% for 5-ASA and 82% for N-acetyl-5-ASA). Metabolism The absorbed mesalamine is extensively metabolized, mainly to N-acetyl-5-ASA in the liver and in the gut mucosal wall. In patients with ulcerative colitis treated with one mesalamine 500 mg rectal suppository every eight hours for six days, the peak concentration (C max ) of N-acetyl-5-ASA ranged from 467 ng/mL to 1399 ng/mL following the initial dose and from 193 ng/mL to 1304 ng/mL at steady state.
Excretion Mesalamine is eliminated from plasma mainly by urinary excretion, predominantly as N-acetyl-5-ASA. In patients with ulcerative proctitis treated with mesalamine 500 mg as a rectal suppository every 8 hours for 6 days, 12% or less of the dose was eliminated in urine as unchanged 5-ASA and 8% to 77% was eliminated as N-acetyl-5-ASA following the initial dose. At steady state, 11% or less of the dose was eliminated in the urine as unchanged 5-ASA and 3% to 35% was eliminated as N-acetyl-5-ASA.
🧬 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, 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 suppositories, USP 1,000 mg for rectal administration are available as off white to light brown opaque bullet shaped suppositories containing 1,000 mg mesalamine, USP. They are supplied as: Carton NDC Unit Dose NDC (Each Suppository) 72 rectal suppositories (12 strips of 6 suppositories) NDC 16571-246-72 NDC 16571-246-16 30 rectal suppositories (5 strips of 6 suppositories) NDC 16571-246-03 NDC 16571-246-16 Store below 25ºC (77ºF), may be refrigerated. Keep away from direct heat, light or humidity.
📋 Description ▾
11 DESCRIPTION The active ingredient in Mesalamine Suppository USP, 1,000 mg for rectal use is mesalamine USP, also known as mesalazine or 5-aminosalicylic acid (5-ASA). Chemically, mesalamine, USP is 5-amino-2-hydroxybenzoic acid, and is classified as an aminosalicylate. Each mesalamine rectal suppository USP contains 1,000 mg of mesalamine, USP in a base of hard fat.
The empirical formula is C 7 H 7 NO 3 , representing a molecular weight of 153.14. The structural formula is: mesalamine-structure.jpg
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION 2Advise patients to read the FDA-approved patient labeling (Patient Information) Administration [see Dosage and Administration ( 2 )] Advise patients: • Do not cut or break the suppository. • Retain the suppository for one to three hours or longer, if possible. • Drink an adequate amount of fluids. • If a dose of mesalamine suppository is missed, administer as soon as possible, unless it is almost time for next dose. Do not use two mesalamine suppositories at the same time to make up for a missed dose. • Urine may become discolored reddish-brown while taking mesalamine suppositories when it comes in contact with surfaces or water treated with hypochlorite-containing bleach.
If discolored urine is observed, advise patients to observe their urine flow. Report to the healthcare provider only if urine is discolored on leaving the body, before contact with any surface or water (e.g., in the toilet). • Mesalamine suppositories will cause staining of direct contact surfaces, including but not limited to fabrics, flooring, painted surfaces, marble, granite, vinyl, and enamel. Keep mesalamine suppositories away from these surfaces to prevent staining.
Renal Impairment • Inform patients that mesalamine suppositories 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 suppositories and report to their healthcare provider if they experience new or worsening symptoms 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 suppositories and report to their healthcare provider at first appearance of a severe cutaneous adverse reaction or any 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 drink an adequate amount of fluids during treatment 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 )]. 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 )]. Manufactured for: Rising Pharma Holdings, Inc. East Brunswick, NJ 08816 Made in India CODE No.: MH/DRUGS/25-KD/724 PIR24672-02 Revised : 06/2025