Clinical Information
Gen. Code and Des.
64701 mesalamine ORAL CAP ER 24H 0.375G
GCN and Des.
16159 mesalamine ORAL CAP ER 24H 0.375G
Strength
Dose Form
CAPSULE, EXT RELEASE 24 HR
Product Category
RX Pharmaceuticals
Fine Line Class
850085008510 All Rx Products
DEA Class
NC
OMP Family
AHFS Class
56360000 ANTI-INFLAMMATORY AGENTS (GI DRUGS)
Active Ingredients
1600 mesalamine 89576
Inactive Ingredients
2537 povidone 9003398
2605 aspartame 22839470
APRISO mesalamine capsule, extended release
DESCRIPTION
Each APRISO capsule is delayed- and extended-release dosage form for oral administration. Each capsule contains 0.375 of mesalamine USP (5-aminosalicylic acid, 5-ASA), an anti-inflammatory drug
Molecular Weight: 153.14
Molecular Formula: C7 H7 NO3
Each APRISO capsule contains granules composed of mesalamine in polymer matrix with an enteric coating that dissolves at pH and above.
The inactive ingredients of APRISO capsules are colloidal silicon dioxide, magnesium stearate, microcrystalline cellulose, simethicone emulsion, ethylacrylate/methylmethacrylate copolymer nonoxynol 100 dispersion, hypromellose, methacrylic acid copolymer, talc, titanium dioxide, triethyl citrate, aspartame, anhydrous citric acid, povidone, vanilla flavor, and edible black ink.
12 CLINICAL PHARMACOLOGY
12.1 Mechanism of Action
The mechanism of action of mesalamine (5-ASA) is unknown, but appears to be local to the intestinal mucosa rather than systemic. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways, i.e., prostanoids, and through the lipoxygenase pathways, i.e., leukotrienes and hydroxyeicosatetraenoic acids, is increased in patients with ulcerative colitis, and it is possible that 5-ASA diminishes inflammation by blocking production of arachidonic acid metabolites.
INDICATIONS AND USAGE
APRISO capsules are indicated for the maintenance of remission of ulcerative colitis in patients 18 years of age and older.
2 DOSAGE AND ADMINISTRATION
The recommended dose for maintenance of remission of ulcerative colitis in adult patients is 1.5 (four APRISO capsules) orally once daily in the morning. APRISO may be taken without regard to meals. APRISO should not be co-administered with antacids. An evaluation of renal function is recommended before initiating therapy with APRISO.
3 DOSAGE FORMS AND STRENGTHS
Extended-release capsules containing 0.375 mesalamine.
4 CONTRAINDICATIONS
APRISO is contraindicated in patients with hypersensitivity to salicylates or aminosalicylates or to any of the components of APRISO capsules.
5 WARNINGS AND PRECAUTIONS
5.1 Renal Impairment
Renal impairment, including minimal change nephropathy, acute and chronic interstitial nephritis, and, rarely, renal failure, has been reported in patients given products such as APRISO that contain mesalamine or are converted to mesalamine.
It is recommended that patients have an evaluation of renal function prior to initiation of APRISO therapy and periodically while on therapy. Exercise caution when using APRISO in patients with known renal dysfunction or history of renal disease.
In animal studies, the kidney was the principal organ for toxicity [See Nonclinical Toxicology 13.2)]
5.2 Mesalamine-Induced Acute Intolerance Syndrome
Mesalamine has been associated with an acute intolerance syndrome that may be difficult to distinguish from flare of inflammatory bowel disease. 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, sometimes fever, headache, and rash. If acute intolerance syndrome is suspected, promptly discontinue treatment with APRISO.
5.3 Hypersensitivity
Some patients who have experienced hypersensitivity reaction to sulfasalazine may have similar reaction to APRISO capsules or to other compounds that contain or are converted to mesalamine.
5.4 Hepatic Impairment
There have been reports of hepatic failure in patients with pre-existing liver disease who have been administered mesalamine. Caution should be exercised when administering APRISO to patients with liver disease.
DRUG INTERACTIONS
Based on in vitro studies, APRISO is not expected to inhibit the metabolism of drugs that are substrates of CYP1A2, CYP2C9, CYP2C19, CYP2D6, or CYP3A4.
7.1 Antacids
Because the dissolution of the coating of the granules in APRISO capsules depends on pH, APRISO capsules should not be co-administered with antacids.
HOW SUPPLIED/STORAGE AND HANDLING
APRISO is available as light blue opaque hard gelatin capsules containing 0.375 mesalamine and with the letters ?G? and ?M? on either side of black band imprinted on the capsule.
NDC 54868-6150-0 Bottles of 120 capsules
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.
