Aminosalicylate

Mesalamine

Approved 19 Apr 2019RectalSuppository

The FDA lists this product in 36 strengths and forms.

Indications

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.

Contraindications

Mesalamine suppositories are 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 or to any ingredients in the formulation. ( 4 , 5 .3 )

Warnings and precautions

Renal Impairment : Evaluate the risks and benefits in patients with known renal impairment or taking nephrotoxic drugs; monitor renal function (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)
Interaction with Laboratory Test for Urinary Normetanephrine : Spuriously elevated test results may occur with liquid chromatography with electrochemical detection in patients receiving MESALAMINE SUPPOSITORIES; use alternative, selective assay for normetanephrine. ( 5.5 , 7.3 )

5.1Renal Impairment

Renal impairment, including minimal change nephropathy, 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 [ see Adverse Reactions (6.2) ] . Evaluate renal function prior to initiation of mesalamine suppositories therapy and periodically while on therapy. Evaluate the risks and benefits of using mesalamine suppositories in patients with known renal impairment or a history of renal disease or taking concomitant nephrotoxic drugs.

In animal studies, the kidney was the principal organ for toxicity [ see Drug Interactions (7.1) , Use in Specific Populations (8.6) and Nonclinical Toxicology (13.2) ] .

At a glance

Brand name: Mesalamine
Pharmacologic class: Aminosalicylate
Route: Rectal
Dosage form: Suppository
Applicant: Rising
Status: Prescription
FDA approval: 19 Apr 2019
Application: ANDA207448-001

Contraindications

Warnings and precautions

Renal Impairment : Evaluate the risks and benefits in patients with known renal impairment or taking nephrotoxic drugs; monitor renal function (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)
Interaction with Laboratory Test for Urinary Normetanephrine : Spuriously elevated test results may occur with liquid chromatography with electrochemical detection in patients receiving MESALAMINE SUPPOSITORIES; use alternative, selective assay for normetanephrine. ( 5.5 , 7.3 )

5.1Renal Impairment

In animal studies, the kidney was the principal organ for toxicity [ see Drug Interactions (7.1) , Use in Specific Populations (8.6) and Nonclinical Toxicology (13.2) ] .

Adverse reactions

The most serious adverse reactions seen in mesalamine suppositories clinical trials or with other products that contain or are metabolized to mesalamine 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) ] The most common adverse reactions (≥ 1%) are: dizziness, rectal pain, fever, rash, acne and colitis. (6.1) To report SUSPECTED ADVERSE REACTIONS, contact Rising Pharmaceuticals, Inc. at 1-866-562-4597 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

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

6.2Postmarketing Experience

In addition to the adverse reactions reported above in clinical trials involving mesalamine suppositories, the adverse reactions listed below have been identified during post-approval use of mesalamine suppositories and 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 nephropathy [ see Warnings and Precautions (5.1) ]
Respiratory, Thoracic and Mediastinal Disorders : hypersensitivity pneumonitis (including allergic alveolitis, eosinophilic pneumonitis, interstitial pneumonitis)
Skin and Subcutaneous Tissue Disorder : alopecia, erythema, erythema nodosum, pruritus, psoriasis, pyoderma gangrenosum, urticaria
Urogenital: reversible oligospermia

Mesalamine

Indications

Contraindications

Warnings and precautions

5.1Renal Impairment

At a glance

Two medicines in one question?

Mesalamine

Indications

Contraindications

Warnings and precautions

5.1Renal Impairment

At a glance

Two medicines in one question?

5.2Mesalamine-Induced Acute Intolerance Syndrome

5.3Hypersensitivity Reactions

5.4Hepatic Failure

5.5Interaction with Laboratory Test for Urinary Normetanephrine Use

Interactions

7.1Nephrotoxic Agents, Including Non-Steroidal Anti-Inflammatory Drugs

7.2Azathioprine or 6-Mercaptopurine

7.3Urinary 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