Mesalamine
FDA Drug Information • Also known as: Apriso, Canasa, Lialda, Mesalamine, Mesalamine Rectal, Pentasa, Rowasa, Sfrowasa Sulfite-Free...
- Brand Names
- Apriso, Canasa, Lialda, Mesalamine, Mesalamine Rectal, Pentasa, Rowasa, Sfrowasa Sulfite-Free Formulation
- Dosage Form
- POWDER
- Product Type
- BULK INGREDIENT
Description
11 DESCRIPTION Each Mesalamine Extended-Release Capsule, USP is a delayed- and extended-release dosage form for oral administration. Each capsule contains 0.375 g of mesalamine USP (5-aminosalicylic acid, 5-ASA), an aminosalicylate. The structural formula of mesalamine is: Molecular Weight: 153.14 Molecular Formula: C 7 H 7 NO 3 Each Mesalamine Extended-Release Capsule, USP contains granules composed of mesalamine in a polymer matrix with an enteric coating that dissolves at pH 6 and above. The inactive ingredients of Mesalamine Extended-Release Capsules, USP are: ethylcellulose, FD&C Blue No. 1, gelatin, hypromellose, methacrylic acid and methyl methacrylate copolymer, silicon dioxide, sodium lauryl sulfate, sugar spheres (corn starch and sucrose), talc, titanium dioxide and triethyl citrate. The imprinting ink has the following ingredients: ferrosoferric oxide, potassium hydroxide and shellac. FDA approved dissolution test specifications differ from USP. Chemical Structure
What Is Mesalamine Used For?
1 INDICATIONS AND USAGE Mesalamine Extended-Release Capsules are indicated for the maintenance of remission of ulcerative colitis in adults. Mesalamine extended-release capsules are an aminosalicylate indicated for the maintenance of remission of ulcerative colitis in adults. ( 1 )
Dosage and Administration
2 DOSAGE AND ADMINISTRATION Dosage The recommended dosage is 1.5 g (four 0.375 g capsules) once daily in the morning. ( 2 ) Administration Instructions Evaluate renal function before initiating therapy with mesalamine extended-release capsules. ( 2 ) Swallow the capsules whole. Do not cut, break, crush or chew the capsules. ( 2 ) Avoid co-administration with antacids. ( 2 , 7.1 ) Drink an adequate amount of fluids. ( 2 , 5.7 ) Take mesalamine extended-release capsules without regard to meals. ( 2 ) Dosage The recommended dosage in adults is 1.5 g (four 0.375 g capsules) orally once daily in the morning. Administration Instructions Evaluate renal function before initiating therapy with mesalamine extended-release capsules [see Warnings and Precautions (5.1) ] . Swallow mesalamine extended-release capsules whole. Do not cut, break, crush or chew the capsules. Avoid co-administration of mesalamine extended-release capsules with antacids [see Drug Interactions (7.1) ] . Drink an adequate amount of fluids [see Warnings and Precautions (5.7) ] . Take mesalamine extended-release capsules without regard to meals [see Clinical Pharmacology (12.3) ] .
Side Effects (Adverse Reactions)
6 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 Upsher-Smith Laboratories, LLC at 1-855-899-9180 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical 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 extended-release capsules in 557 patients, including 354 exposed for at least 6 months and 250 exposed for greater than one year. Mesalamine extended-release capsules were studied in two placebo-controlled trials (n=367 treated with mesalamine extended-release capsules) 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 extended-release capsules 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 extended-release capsules-treated patients and at a greater rate than placebo are shown in Table 1 below. Table 1: Common Adverse Reactions Reported in at least 3% of mesalamine extended-release capsules-treated patients and at a greater rate than with placebo. in Clinical Trials of Adults with Ulcerative Colitis Mesalamine Extended-Release Capsules 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% The following adverse reactions, presented by body system, were reported at a frequency less than 3% in patients treated with mesalamine extended-release capsules 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 6.2 Postmarketing Experience The following adverse reactions have been identified during post approval use of mesalamine extended-release capsules or other mesalamine-containing 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...
Drug Interactions
7 DRUG INTERACTIONS Nephrotoxic Agents including NSAIDs : Increased risk of nephrotoxicity; monitor for changes in renal function and mesalamine-related adverse reactions. ( 7.2 ) Azathioprine or 6-Mercaptopurine : Increased risk of blood disorders; monitor complete blood cell counts and platelet counts. ( 7.3 ) 7.1 Antacids Because the dissolution of the coating of the granules in mesalamine extended-release capsules depends on pH, avoid co-administration of mesalamine extended-release capsules with antacids [see Dosage and Administration (2) ] . 7.2 Nephrotoxic Agents, Including Non-Steroidal Anti-Inflammatory Drugs The concurrent use of mesalamine with known nephrotoxic agents, including non-steroidal 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) ] . 7.3 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 extended-release capsules and azathioprine or 6-mercaptopurine cannot be avoided, monitor blood tests, including complete blood cell counts and platelet counts. 7.4 Interference with Urinary Normetanephrine Measurements Use of mesalamine extended-release capsules may lead to spuriously elevated test results when measuring urinary normetanephrine by liquid chromatography with electrochemical detection [see Warnings and Precautions (5.9) ] . Consider an alternative, selective assay for normetanephrine.
Contraindications
4 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 capsules. ( 4 , 5.3 )
Pregnancy and Breastfeeding
8.1 Pregnancy 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 2,500 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...
Overdosage
10 OVERDOSAGE Mesalamine extended-release capsules are an aminosalicylate, and symptoms of salicylate toxicity include nausea, vomiting and abdominal pain, tachypnea, hyperpnea, tinnitus, and neurologic symptoms (headache, dizziness, confusion, seizures). Severe salicylate intoxication may lead to electrolyte and blood pH imbalance and potentially to other organ (e.g., renal and liver) damage. There is no specific antidote for mesalamine overdose; however, conventional therapy for salicylate toxicity may be beneficial in the event of acute overdosage and may include gastrointestinal tract decontamination to prevent further absorption. Correct fluid and electrolyte imbalance by the administration of appropriate intravenous therapy and maintain adequate renal function. Mesalamine extended-release capsules are a pH-dependent delayed-release product and this factor should be considered when treating a suspected overdose.
How Supplied
16 HOW SUPPLIED/STORAGE AND HANDLING Mesalamine Extended-Release Capsules, USP, 0.375 g are available as follows: Capsule with opaque powder blue cap and body, imprinted with ' ' on cap and '375' on body in black ink, containing light pink or light tan pellets. Bottles of 120 capsules with a child-resistant closure, NDC 0832-6056-12 Image Storage : Store at 20° to 25°C (68° to 77°F); excursions permitted between 15° and 30°C (59° and 86°F) [See USP Controlled Room Temperature]. Dispense in a tight, light-resistant container as defined in the USP with a child-resistant closure. Keep out of reach of children.
About This Information
This drug information is sourced from FDA-approved labeling via the openFDA database. It is intended for educational and reference purposes only. This is not medical advice. Always consult your healthcare provider before making decisions about medication. Drug information may be updated by the FDA; check with your pharmacist for the most current information.
What are side effects?
Side effects are unwanted reactions that can occur when taking a medication. They range from mild (headache, nausea) to severe (allergic reactions, organ damage). Not everyone experiences side effects, and severity varies. Report any concerning side effects to your doctor.
What are drug interactions?
Drug interactions occur when a medication is affected by another drug, food, or supplement. Interactions can make medications less effective or cause dangerous side effects. Always tell your doctor about all medications and supplements you take.