Two double-blind, placebo-controlled, multicenter trials of mesalamine suppositories were conducted in North America in adult patients with mildly to moderately active ulcerative proctitis. The regimen in Study 1 was a 500 mg mesalamine suppository administered rectally three times daily and in Study 2 was a 500 mg mesalamine suppository administered rectally twice daily. In both trials, patients had an average extent of proctitis (upper disease boundary) of approximately 10 cm and approximately 80% of patients had multiple prior episodes of proctitis. A total of 173 patients were evaluated (Study 1, N=79; Study 2, N=94), of which 89 patients received mesalamine, and 84 patients received placebo. The mean age of patients was 39 years (range 17 to 73 years), 60% were female, and 97% were white.
The primary measures of efficacy were clinical disease activity index (DAI) and histologic evaluations in both trials. The DAI is a composite index reflecting rectal bleeding, stool frequency, mucosal appearance at endoscopy, and a physician’s global assessment of disease. Patients were evaluated clinically and sigmoidoscopically after 3 and 6 weeks of treatment.
Compared to placebo, mesalamine suppositories were statistically (p<0.01) superior to placebo in both trials with respect to improvement in stool frequency, rectal bleeding, mucosal appearance, disease severity, and overall disease activity after 3 and 6 weeks of treatment. The effectiveness of mesalamine suppositories was statistically significant irrespective of sex, extent of proctitis, duration of current episode, or duration of disease.
An additional multicenter, open-label, randomized, parallel group study in 99 patients diagnosed with mildly to moderately ulcerative proctitis compared 1000 mg mesalamine administered rectally once daily at bedtime (N=35) to 500 mg mesalamine suppository administered rectally twice daily, in the morning and at bedtime (N=46), for 6 weeks.
The primary measures of efficacy included the clinical disease activity index (DAI) and histologic evaluations. Patients were evaluated clinically and sigmoidoscopically at 3 and 6 weeks of treatment.
The efficacy at 6 weeks was not different between the treatment groups. Both were effective in the treatment of ulcerative proctitis and resulted in a significant decrease at 6 weeks in DAI: in the mesalamine 500 mg twice daily group, the mean DAI value decreased from 6.6 to 1.6, and in the 1000 mg at bedtime group, the mean DAI value decreased from 6.2 to 1.3, which represents a decrease of greater than 75% in both groups. After 6 weeks of treatment, a DAI score of less than 3 was achieved in 78% of patients in the mesalamine 500 mg twice daily group and 86% of patients in the mesalamine 1000 mg once daily group. The recommended dosage of mesalamine is 1000 mg administered rectally once daily at bedtime [see Dosage and Administration ( 2)].
16 HOW SUPPLIED/STORAGE AND HANDLING
Mesalamine 1000 mg suppositories for rectal administration are available as bullet shaped, light tan to grey suppositories containing 1000 mg mesalamine supplied in boxes of 30 individually plastic wrapped suppositories (NDC 59762-0118-3).
Store below 25ºC (77ºF), may be refrigerated. Keep away from direct heat, light or humidity.
Advise patients to read the FDA-approved patient labeling (Patient Information)
Administration [see Dosage and Administration (2)]
- 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 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.
- Inform patients that mesalamine 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 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)].
- 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)].
- 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 ( 5.5)].
- 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 ( 5.6) ].
- 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)].
© 2020 Allergan. All rights reserved.
Patented. See www.allergan.com/patents
For more information, go to www.greenstonellc.com or call 1-800-438-1985
|PATIENT INFORMATION M esalamine suppositories, for rectal use|
|What is mesalamine ? Mesalamine is a prescription medicine used to treat adults with active ulcerative proctitis (ulcerative rectal colitis).It is not known if mesalamine is safe and effective in children.|
|Do not use mesalamine if you are: |
|Before using mesalamine , tell your doctor if you have any medical conditions, including if you : |
| How should I take mesalamine ? |
| What are the possible side effects of mesalamine ? M esalamine may cause serious side effects, including: |
|o cramps||o fever|
|o stomach (abdominal) pain||o headache|
|o bloody diarrhea||o rash|
|o chest pain||o shortness of breath|
|o decrease in the amount of urineo eye inflammation||o fatigue|
|o yellowing of your eyes||o flu-like symptoms|
|o itchy skin||o nausea or vomiting|
|o feeling very tired|
|o dizziness||o rectal pain|
|o acne||o fever|
|o inflammation of the large intestine (colitis)||o rash|
|These are not all of the possible side effects of mesalamine. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.|
| How should I store mesalamine ? |
|General information about the safe and effective use of mesalamine . Medicines are sometimes prescribed for purposes other than those listed in a Patient Information leaflet. Do not use mesalamine for a condition for which it was not prescribed. Do not give mesalamine to other people, even if they have the same symptoms that you have. It may harm them.You can ask your pharmacist or healthcare provider for information about mesalamine that is written for health professionals.|
|What are the ingredients in mesalamine ? Active ingredients: mesalamineInactive ingredients: hard fat baseDistributed by: Greenstone LLC, Peapack, NJ 07977© 2020 Allergan. All rights reserved. Patented. See www.allergan.com/patents.For more information, go to www.greenstonellc.com or call 1-800-438-1985.|
This Patient Information has been approved by the U.S. Food and Drug Administration Revised: October 2020
RxDrugLabels.com provides trustworthy package insert and label information about marketed prescription drugs as submitted by manufacturers to the U.S. Food and Drug Administration. Package information is not reviewed or updated separately by RxDrugLabels.com. Every individual prescription drug label and package insert entry contains a unique identifier which can be used to secure further details directly from the U.S. National Institutes of Health and/or the FDA.