Overview
11 DESCRIPTION The active ingredient in DIPENTUM (olsalazine sodium) is the sodium salt of a salicylate, disodium 3,3'-azobis (6-hydroxybenzoate) a compound that is effectively bioconverted to mesalamine (5-aminosalicylic acid,5-ASA), an aminosalicylate. Its empirical formula is C14H8N2Na2O6 with a molecular weight of 346.21.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Upon reaching the colon, colonic bacteria convert olsalazine into 5‑aminosalicylic acid (5-ASA or mesalazine). The mechanism of action of 5-ASA (mesalamine) is not fully understood, but appears to be a topical anti-inflammatory effect on colonic epithelial cells. 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 mesalamine diminishes inflammation by blocking cyclooxygenase and inhibiting prostaglandin production in the colon. 12.
Indications
- 1 INDICATIONS AND USAGE DIPENTUM is indicated for the maintenance of remission of ulcerative colitis in adult patients who are intolerant of sulfasalazine. DIPENTUM is an aminosalicylate indicated for the maintenance of remission of ulcerative colitis in adult patients who are intolerant of sulfasalazine. ( 1 )
Common Doses
- 500 mg
Dosage
2 DOSAGE AND ADMINISTRATION Evaluate renal function before initiating therapy with DIPENTUM [see Warnings and Precautions (5.1) ]. The recommended dosage is 500 mg orally twice daily. Drink an adequate amount of fluids during treatment [see Warnings and Precautions (5.7) ] . • Evaluate renal function prior to initiation of DIPENTUM and periodically while on therapy. ( 2 , 5.1 ) • The recommended dosage is 500 mg orally twice daily. ( 2 ) • Drink an adequate amount of fluids. ( 2 , 5.7 )
Contraindications
- 4 CONTRAINDICATIONS DIPENTUM is contraindicated in patients with known or suspected hypersensitivity to salicylates, aminosalicylates, or to any of the excipients in DIPENTUM [see Warnings and Precautions (5.3) , Description (11) ] . Known or suspected hypersensitivity to salicylates or aminosalicylates or to any of the ingredients of DIPENTUM. ( 4 , 5.3 )
Side Effects
- 6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the 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.
Interactions
- 7 DRUG INTERACTIONS • Nephrotoxic Agents including Non-Steroidal Anti-inflammatory Drugs (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 dyscrasias; monitor complete blood cell counts and platelet counts. ( 7.2 ) • Low Molecular Weight Heparins or Heparinoids : Increased risk of bleeding following neuraxial anesthesia; if possible, discontinue DIPENTUM or closely monitor for bleeding. ( 7.