Drug Facts
Composition & Profile
Identifiers & Packaging
16 HOW SUPPLIED/STORAGE AND HANDLING Mesalamine suppositories, 1,000 mg for rectal administration are available as bullet shaped, light tan to grey suppositories containing 1,000 mg mesalamine packed in PVC/PE molds. They are suppled as follows: Carton of 30 rectal suppositories (5 strips of 6 suppositories) NDC 31722-005-30 Carton of 42 rectal suppositories (7 strips of 6 suppositories) NDC 31722-005-31 Store below 25ºC (77ºF), may be refrigerated. Keep away from direct heat, light or humidity.; PACKAGE LABEL.PRINCIPAL DISPLAY PANEL Mesalamine Rectal Suppositories 1,000 mg 30s Carton Mesalamine Rectal Suppositories 1,000 mg 42s Carton Mesalamine Rectal Suppositories 1,000 mg Foil front view Mesalamine Rectal Suppositories 1,000 mg Foil rear view mesalaminerectalsupp-1000mgcarton-30scount mesalaminerectalsupp-1000mgcarton-42scount mesalaminerectalsupp1000mg-foilfrontview mesalaminerectalsupp-1000mgfoilrearview
- 16 HOW SUPPLIED/STORAGE AND HANDLING Mesalamine suppositories, 1,000 mg for rectal administration are available as bullet shaped, light tan to grey suppositories containing 1,000 mg mesalamine packed in PVC/PE molds. They are suppled as follows: Carton of 30 rectal suppositories (5 strips of 6 suppositories) NDC 31722-005-30 Carton of 42 rectal suppositories (7 strips of 6 suppositories) NDC 31722-005-31 Store below 25ºC (77ºF), may be refrigerated. Keep away from direct heat, light or humidity.
- PACKAGE LABEL.PRINCIPAL DISPLAY PANEL Mesalamine Rectal Suppositories 1,000 mg 30s Carton Mesalamine Rectal Suppositories 1,000 mg 42s Carton Mesalamine Rectal Suppositories 1,000 mg Foil front view Mesalamine Rectal Suppositories 1,000 mg Foil rear view mesalaminerectalsupp-1000mgcarton-30scount mesalaminerectalsupp-1000mgcarton-42scount mesalaminerectalsupp1000mg-foilfrontview mesalaminerectalsupp-1000mgfoilrearview
Overview
The active ingredient in mesalamine 1,000 mg suppositories for rectal use is mesalamine, also known as mesalazine or 5-aminosalicylic acid (5-ASA). Chemically, mesalamine is 5-amino-2-hydroxybenzoic acid, and is classified as an aminosalicylate. Each mesalamine rectal suppository contains 1,000 mg of mesalamine USP in a base of Hard Fat, NF. The molecular formula is C 7 H 7 NO 3 , representing a molecular weight of 153.14. The structural formula is: mesalaminerectalsupp-structure
Indications & 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 & 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 suppositories 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 suppositories 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 )
Warnings & Precautions
• Renal Impairment : Evaluate the risks and benefits in patients with known renal impairment or taking nephrotoxic drugs; monitor renal function. Discontinue mesalamine 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 suppositories; use alternative, selective assay for normetanephrine. ( 5.8 ) 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 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 suppository 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. Discontinue mesalamine suppositories if renal function deteriorates while on therapy. [see 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, 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 suppositories. 5.3 Hypersensitivity 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. 5.4 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 suppositories in patients with known liver impairment. 5.5 Severe Cutaneous Adverse Reactions Severecutaneous adverse reactions, including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN), drug reaction with eosinophilia andsystemicsymptoms (DRESS), and acute generalized exanthematous pustulosis (AGEP) have been reported in association with the use ofmesalamine [see Adverse Reactions ( 6.2 )]. Discontinue mesalamine suppositories at the first signs or symptoms of severe cutaneous adverse reactions or other signs of hypersensitivity and considerfurtherevaluation. 5.6 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. 5.7 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 suppositories. 5.8 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.
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 ingredients in the formulation. ( 4 , 5.3 )
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 Annora Pharma Private Limited at 1-866-495-1995 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch 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 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 suppositories is 1,000 mg administered rectally once daily at bedtime [see Dosage and Administration ( 2 )]. 6.2 Postmarketing 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 alveolitis, eosinophilic pneumonitis, interstitial pneumonitis), pleuritis/pleurisy • Skin and Subcutaneous Tissue Disorder : alopecia, erythema, erythema nodosum, pruritus, psoriasis, pyoderma gangrenosum, urticaria, SJS/TEN, DRESS and AGEP [see Warnings and Precautions ( 5.5 )] • Urogenital : reversible oligospermia
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 ) 7.1 Nephrotoxic 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 )]. 7.2 Azathioprine 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 suppositories and azathioprine or 6-mercaptopurine cannot be avoided, monitor blood tests, including complete blood cell counts and platelet counts. 7.3 Interference 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 )].
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