MESALAMINE- mesalamine suppository
Greenstone LLC


Mesalamine is indicated in adults for the treatment of mildly to moderately active ulcerative proctitis.



The recommended dosage of mesalamine in adults is 1000 mg administered rectally once daily at bedtime for 3 to 6 weeks depending on symptoms and sigmoidoscopic findings. Safety and effectiveness of mesalamine beyond 6 weeks have not been established.

Administration Instructions:

• Evaluate renal function prior to initiation of mesalamine 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 ( 5.6)].

• If a dose of mesalamine 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 away from these surfaces to prevent staining.


Mesalamine Suppository: 1000 mg in a bullet shaped, light tan to grey suppository.


Mesalamine is contraindicated in patients with known or suspected hypersensitivity to salicylates or aminosalicylates or to any ingredients in the suppository vehicle [ s ee Warnings and Precautions ( 5.3), Adverse Reactions ( 6.2), and Description ( 11)].


5.1 Renal Impairment

Renal impairment, including minimal change disease, acute and chronic interstitial nephritis, and renal failure, has been reported in patients given products 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 therapy 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 [ s ee Drug Interactions ( 7.1) , Use in Specific Populations ( 8.6) ] .

5.2 Mesalamine-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, pruritis, conjunctivitis, and rash. Monitor patients for worsening of these symptoms while on treatment. If acute intolerance syndrome is suspected, promptly discontinue treatment with mesalamine.

5.3 Hypersensitivity 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.

5.4 Hepatic 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.

5.5 Photosensitivity

In patients treated with mesalamine or sulfasalazine who have pre-existing skin conditions such as atopic dermatitis and atopic eczema have reported more severe photosensitivity reactions. Advise patients to avoid sun exposure, wear protective clothing, and use a broad-spectrum sunscreen when outdoors.

5.6 Nephrolithiasis

Cases of nephrolithiasis have been reported with the use of mesalamine, including stones of 100% mesalamine content. Mesalamine-containing stones are radiotransparent and undetectable by standard radiography or computed tomography (CT). Ensure adequate hydration during treatment with mesalamine.

5. 7 Interaction with Laboratory Test for Urinary Normetanephrine

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.


The following serious or clinically significant adverse reactions are described elsewhere in labeling:

  • Renal Impairment [ s ee Warnings and Precautions ( 5.1)]
  • Mesalamine-Induced Acute Intolerance Syndrome [ s ee Warnings and Precautions ( 5.2)]
  • Hypersensitivity Reactions [ s ee Warnings and Precautions ( 5.3)]
  • Hepatic Failure [ s ee Warnings and Precautions ( 5.4)]
  • Photosensitivity [see Warnings and Precautions ( 5.5)]
  • Nephrolithiasis [see Warnings and Precautions ( 5.6)]

6.1 Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

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 2.4
Rectal 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 1000 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 is 1000 mg administered rectally once daily at bedtime [see Dosage and Administration ( 2)].

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