Generic Name
Mesalamine
Brand Names
Pentasa, Apriso, Canasa, Lialda, Rowasa, sfRowasa Sulfite-Free
FDA approval date: May 10, 1993
Classification: Aminosalicylate
Form: Suppository, Tablet, Enema, Kit, Suspension, Capsule
What is Pentasa (Mesalamine)?
Mesalamine delayed-release tablets are indicated for the: induction and maintenance of remission in adult patients with mildly to moderately active ulcerative colitis. Pediatric use information is approved for Takeda Pharmaceuticals U.S.A., Inc.'s LIALDA delayed-release tablets. However, due to Takeda Pharmaceuticals U.S.A., Inc.'s marketing exclusivity rights, this drug product is not labeled with that information. Mesalamine delayed-release tablets are an aminosalicylate indicated for the: induction and maintenance of remission in adult patients with mildly to moderately active ulcerative colitis.
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Brand Information
Pentasa (mesalamine)
1INDICATIONS AND USAGE
PENTASA is indicated for the induction of remission and for the treatment of mildly to moderately active ulcerative colitis in adult patients.
2DOSAGE AND ADMINISTRATION
Evaluate renal function prior to initiation of PENTASA and periodically while on therapy
Recommended Dosage
The recommended dosage for the induction of remission and the symptomatic treatment of mildly to moderately active ulcerative colitis in adults is 1 g (4 PENTASA 250 mg capsules or 2 PENTASA 500 mg capsules) administered orally four times daily.
Administration Instructions
- Swallow PENTASA capsules whole; do not crush or chew.
- Alternatively, the capsule(s) may be opened and the entire contents sprinkled onto applesauce or yogurt. Consume the entire mixture immediately.
- Drink an adequate amount of fluids during treatment
3DOSAGE FORMS AND STRENGTHS
Extended-release capsules
- 250 mg as a green and blue capsule imprinted with a pentagonal starburst logo and the number 2010 on the green portion of the capsule and S429 250 mg on the blue portion of the capsule.
- 500 mg as a blue capsule imprinted with a pentagonal starburst logo and S429 500 mg.
4CONTRAINDICATIONS
PENTASA is contraindicated in patients with known or suspected hypersensitivity to salicylates, aminosalicylates, or any ingredients of PENTASA
5ADVERSE REACTIONS
The following clinically significant adverse reactions are described elsewhere in the labeling:
- Renal impairment
- Mesalamine-induced acute intolerance syndrome
- Hypersensitivity reactions
- Hepatic failure
- Severe cutaneous adverse reactions
- Photosensitivity
- Nephrolithiasis
5.1Clinical 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.
More than 2100 patients were exposed to PENTASA in clinical trials of ulcerative colitis or another gastrointestinal condition. The most common adverse reactions (i.e., greater than or equal to 1%) were diarrhea (3%), headache (2%), nausea (2%), abdominal pain (2%), dyspepsia (2%), vomiting (2%), and rash (1%).
The safety of PENTASA was evaluated in two randomized, double-blind, placebo-controlled, dose-response trials (UC-1 and UC-2) of 624 patients with mildly to moderately active ulcerative colitis for up to 8 weeks of treatment
The following adverse reactions, presented by body system, were reported in less than 1% of patients in UC-1, UC-2, and clinical trials for another gastrointestinal condition.
Blood and lymphatic system disorders: thrombocythemia, thrombocytopenia
Cardiac Disorders: palpitations, pericarditis, vasodilation
Gastrointestinal Disorders: abdominal distention, constipation, duodenal ulcer, dysphagia, eructation, esophageal ulcer, fecal incontinence, GI bleeding, mouth ulcer, pancreatitis, rectal bleeding, stool abnormalities (color or texture change)
General disorders and administration site conditions: fever, malaise
Infections and infestations: oral moniliasis, conjunctivitis
Investigations: GGTP increase, increased alkaline phosphatase, LDH increase, SGOT increase, SGPT increase, lipase increase, amylase increase
Metabolism and nutritional disorders: anorexia, edema, thirst
Musculoskeletal and connective tissue disorders: arthralgia, leg cramps, myalgia
Nervous System Disorders: dizziness, insomnia, somnolence, paresthesia
Psychiatric disorders: depression, asthenia
Renal and urinary disorders: albuminuria, hematuria, urinary frequency
Reproductive system and breast disorders: amenorrhea, breast pain, hypomenorrhea, menorrhagia, metrorrhagia
Respiratory, Thoracic and Mediastinal Disorders: pulmonary infiltrates, one week after completion of an 8-week ulcerative colitis study, a 72-year-old male, with no previous history of pulmonary problems, developed dyspnea. The patient was subsequently diagnosed with interstitial pulmonary fibrosis without eosinophilia by one physician and bronchiolitis obliterans with organizing pneumonitis by a second physician.
Skin and Subcutaneous Tissue Disorders: acne, alopecia, dry skin, eczema, erythema nodosum, nail disorder, photosensitivity, pruritus, sweating, urticaria, ecchymosis, lichen planus
5.2Postmarketing Experience
The following adverse reactions have been identified during post-approval use of mesalamine. 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.
Cardiac Disorders: chest pain, fatal myocarditis, pericarditis, T-wave abnormalities
Hematologic Disorders: agranulocytosis, anemia, aplastic anemia, leukopenia, pancytopenia
Hepatic Disorders: cirrhosis, jaundice, including cholestatic jaundice; hepatotoxicity, hepatitis, and possible hepatocellular damage including liver necrosis and liver failure. Some of these cases were fatal. One case of Kawasaki-like syndrome which included hepatic function changes was also reported.
Immune System Disorders: anaphylactic reaction, angioedema, lupus-like syndrome, systemic lupus erythematosus
Nervous System Disorders: intracranial hypertension
Renal and Urinary Disorders: acute renal failure, chronic renal failure, interstitial nephritis, nephrogenic diabetes insipidus, nephrolithiasis, nephrotic syndrome [see
- Urine discoloration occurring ex-vivo caused by contact of mesalamine, including inactive metabolite, with surfaces or water treated with hypochlorite-containing bleach
Reproductive System and Breast Disorders: reversible oligospermia
Respiratory, Thoracic and Mediastinal Disorders: hypersensitivity pneumonitis (including interstitial pneumonitis, allergic alveolitis, eosinophilic pneumonitis), interstitial lung disease, pleurisy/pleuritis, pneumonitis
Skin and Subcutaneous Tissue Disorders: AGEP, DRESS, SJS/TEN [see
6OVERDOSAGE
PENTASA is an aminosalicylate, and symptoms of salicylate toxicity may be possible, such as: nausea, vomiting, abdominal pain, tachypnea, hyperpnea, tinnitus, and neurologic symptoms (headache, dizziness, confusion, seizures). Severe intoxication with salicylates 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.
7DESCRIPTION
PENTASA (mesalamine) for oral administration is an extended-release formulation of mesalamine, an aminosalicylate anti-inflammatory agent for gastrointestinal use.
Mesalamine (also referred to as 5-aminosalicylic acid or 5-ASA) has the chemical name 5-amino-2-hydroxybenzoic acid. It has a molecular weight of 153.14.
The structural formula is:
Each 250 mg capsule contains 250 mg of mesalamine. It also contains the following inactive ingredients: acetylated monoglyceride, castor oil, colloidal silicon dioxide, ethylcellulose, hydroxypropyl methylcellulose, starch, stearic acid, sugar, talc, and white wax. The capsule shell contains D&C Yellow #10, FD&C Blue #1, FD&C Green #3, gelatin, titanium dioxide, and other ingredients.
Each 500 mg capsule contains 500 mg of mesalamine. It also contains the following inactive ingredients: acetylated monoglyceride, castor oil, colloidal silicon dioxide, ethylcellulose, hydroxypropyl methylcellulose, starch, stearic acid, sugar, talc, and white wax. The capsule shell contains FD&C Blue #1, gelatin, titanium dioxide, and other ingredients.
8CLINICAL STUDIES
In two randomized, double-blind, placebo-controlled, dose-response trials (UC-1 and UC-2) of 625 patients with active mild to moderate ulcerative colitis, PENTASA, at an oral dose of 1 g administered four times a day for up to 8 weeks, produced consistent improvement in prospectively identified primary efficacy parameters, Physical Global Assessment, Treatment Failure, and Sigmoidoscopic Index as shown in
A PENTASA dosage regimen of 1 g four times a day demonstrated consistent improvement in secondary efficacy parameters, namely the frequency of trips to the toilet, stool consistency, rectal bleeding, abdominal/rectal pain, and urgency. A PENTASA dosage regimen of 1 g four times a day also induced remission as assessed by endoscopic and symptomatic endpoints.
9HOW SUPPLIED/STORAGE AND HANDLING
PENTASA (mesalamine) extended-release capsules are supplied as shown in the table:
10PRINCIPAL DISPLAY PANEL - 250 mg Capsule Bottle Label
189-81
Pentasa
Extended-Release
240 CAPSULES
Rx only
250 mg
Takeda
11PRINCIPAL DISPLAY PANEL - 500 mg Capsule Bottle Label
191-12
Pentasa
Extended-Release
120 CAPSULES
Rx only
500 mg
Takeda
