Aminosalicylate

Mesalamine

Approved 28 Oct 2022OralCapsule, extended release

The FDA lists this product in 36 strengths and forms.

Indications

Mesalamine extended-release capsules are indicated for the maintenance of remission of ulcerative colitis in adults. Mesalamine extended-release capsule is an aminosalicylate indicated for the maintenance of remission of ulcerative colitis in adults. (1)

Contraindications

Mesalamine extended-release capsules are contraindicated in patients with hypersensitivity to salicylates or aminosalicylates or to any of the components of mesalamine extended-release capsules [see Warnings and Precautions (5.3), Adverse Reactions (6.2), Description (11)]. Known or suspected hypersensitivity to salicylates, aminosalicylates, or any component of mesalamine extended-release capsule. (4, 5.3)

Warnings and precautions

Renal Impairment: Assess renal function at the beginning of treatment and periodically during treatment. Evaluate the risks and benefits in patients with known renal impairment or taking nephrotoxic drugs; monitor renal function. (5.1, 7.2, 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 fluid intake during treatment. (5.7)

Contraindications

Warnings and precautions

Renal Impairment: Assess renal function at the beginning of treatment and periodically during treatment. Evaluate the risks and benefits in patients with known renal impairment or taking nephrotoxic drugs; monitor renal function. (5.1, 7.2, 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 fluid intake during treatment. (5.7)

Pregnancy and breastfeeding

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) . In animal reproduction studies, there were no adverse developmental outcomes with administration of oral mesalamine during organogenesis to pregnant rats and rabbits at doses 1.7 and 5.4 times, respectively, the maximum recommended human 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. 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 in 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, and 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 rats at oral doses up to 320 mg/kg/day (about 1.7 times the recommended human dose based on a body surface area comparison) and rabbits at doses up to 495 mg/kg/day (about 5.4 times the recommended human dose based on a body surface area comparison) and have revealed no evidence of harm to the fetus due to mesalamine.

Adverse reactions

The following 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)] Most common adverse reactions (≥3%) are: headache, diarrhea, upper abdominal pain, nausea, and nasopharyngitis. (6.1) To report SUSPECTED ADVERSE REACTIONS, contact FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

6.1Clinical Trials Experience

Because clinical studies 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 data described below reflect exposure to mesalamine in 557 patients, including 354 exposed for at least 6 months and 250 exposed for greater than one year.

Mesalamine was studied in two placebo-controlled trials (n=367 treated with mesalamine) and in one open-label, long-term study (n=190 additional patients). The population consisted of patients with ulcerative colitis; the mean age was 47 years, 54% were female, and 93% were white. Patients received doses of mesalamine 1.5 g administered orally once per day for six months in the placebo-controlled trials and for up to 24 months in the open-label study.

In the two placebo-controlled trials, the most common reactions reported in at least 3% of mesalamine-treated patients and at a greater rate than placebo are shown in Table 1 below. Table 1: Common Adverse Reactions* in Clinical Trials of Adults with Ulcerative Colitis Mesalamine 1.5 g once daily N=367 Placebo N=185 Headache 11% 8% Diarrhea 8% 7% Upper Abdominal Pain 5% 3% Nausea 4% 3% Nasopharyngitis 4% 3% * Reported in at least 3% of mesalamine-treated patients and at a greater rate than with placebo The following adverse reactions, presented by body system, were reported at a frequency less than 3% in patients treated with mesalamine for up to 24 months in controlled and open-label trials.

Ear and Labyrinth Disorders : tinnitus, vertigo Dermatological Disorder : alopecia Gastrointestinal : lower abdominal pain, rectal hemorrhage Laboratory Abnormalities : increased triglycerides, decreased hematocrit and hemoglobin General Disorders and Administration Site Disorders : fatigue Hepatic : hepatitis cholestatic, transaminases increased Renal Disorders : creatinine clearance decreased, hematuria Musculoskeletal : pain, arthralgia Respiratory : dyspnea

6.2Postmarketing Experience

The following adverse reactions have been identified during post approval use of mesalamine or other mesalaminecontaining products. Because many of these reactions are reported voluntarily from a population of unknown size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Body as a Whole : lupus-like syndrome, drug fever Cardiovascular : pericarditis, pericardial effusion, myocarditis [see Warnings and Precautions (5.3)] Gastrointestinal : pancreatitis, cholecystitis, gastritis, gastroenteritis, gastrointestinal bleeding, perforated peptic ulcer Hepatic : jaundice, cholestatic jaundice, hepatitis, liver necrosis, liver failure, Kawasaki-like syndrome including changes in liver enzymes Hematologic : agranulocytosis, aplastic anemia Nervous System : intracranial hypertension Neurological/Psychiatric : peripheral neuropathy, Guillain-Barré syndrome, transverse myelitis Renal and Urinary : nephrogenic diabetes insipidus, interstitial nephritis, renal failure, minimal change disease, nephrolithiasis [see Warnings and Precautions (5.1, 5.7)] Respiratory/Pulmonary : eosinophilic pneumonia, interstitial pneumonitis, pleurisy/pleuritis Skin : psoriasis, pyoderma gangrenosum, erythema nodosum, SJS/TEN, DRESS, and AGEP [see Warnings and Precautions (5.5)] Renal/Urogenital : reversible oligospermia

Mesalamine

Indications

Contraindications

Warnings and precautions

Two medicines in one question?

Mesalamine

Indications

Contraindications

Warnings and precautions

Two medicines in one question?

5.1Renal Impairment

5.2Mesalamine-Induced Acute Intolerance Syndrome

5.3Hypersensitivity Reactions

5.4Hepatic Failure

5.5Severe Cutaneous Adverse Reactions

5.6Photosensitivity Patients

5.7Nephrolithiasis Cases

5.9Interference with Laboratory Tests Use

Interactions

7.1Antacids Because

7.2Nephrotoxic Agents, Including Non-Steroidal Anti-Inflammatory Drugs

7.3Azathioprine or 6-Mercaptopurine

7.4Interference with Urinary Normetanephrine Measurements Use

Pregnancy and breastfeeding

8.1Pregnancy Risk Summary

Adverse reactions

6.1Clinical Trials Experience

6.2Postmarketing Experience

Composition

Strengths and forms

Official product information

At a glance