Inflammatory bowel disease
Balsalazide (colazal ® )
| Indication: treatment of mildly to moderately active ulcerative colitis. Safety and effectiveness of Colazal ® beyond 12 weeks has not been established.
Dosing (Adults): Usual dose: three 750 mg capsules taken three times a day for a total daily dose of 6.75 grams for a duration of 8 weeks. Some patients in the clinical trials required treatment for up to 12 weeks. [Supplied: 750mg capsule] |
Balsalazide disodium - giazo®
| Drug UPDATES: GIAZO (balsalazide disodium) tablets, for oral use [Drug information ] Dosing: Click (+) next to Dosage and Administration section (drug info link) ABBREVIATED MONOGRAPH - SEE PACKAGE INSERT. Initial U.S. Approval: 2012 Mechanism of Action: Balsalazide is a prodrug of mesalamine (5-aminosalicylic acid, 5-ASA). The mechanism of action of 5-ASA is unknown, but appears to be local to the colonic 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 in the colon. INDICATIONS AND USAGE Limitations of Use DOSAGE AND ADMINISTRATION CONTRAINDICATIONS |
Budesonide (entocort ec ®, uceris® )
| INDICATIONS AND USAGE ENTOCORT EC is indicated for 1] the treatment of mild to moderate active Crohn's disease involving the iluem and/or the ascending colon and 2] the maintenance of clinical remission of mild to moderate Crohn's disease involving the ileum and/or the ascending colon for up to 3 months UCERIS® (budesonide) extended release tablets, for oral use DOSAGE AND ADMINISTRATION UCERIS® DOSAGE FORMS AND STRENGTHS: ------------------------New Product:--------------------------------------------------- Drug: UCERIS® (budesonide) rectal foam U.S. Approval: 2014 Mechanism of Action: Budesonide has glucocorticosteroid (GCS) activity. INDICATIONS AND USAGE: UCERIS rectal foam is a glucocorticosteroid indicated for the induction of remission in patients with active mild to moderate distal ulcerative colitis extending up to 40 cm from the anal verge. DOSAGE AND ADMINISTRATION 2.2 Administration Instructions HOW SUPPLIED: UCERIS rectal foam contains 2 mg budesonide per metered dose.
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Infliximab (remicade ®)
| CLINICAL PHARMACOLOGY General Infliximab neutralizes the biological activity of TNFα by binding with high affinity to the soluble and transmembrane forms of TNFα and inhibits binding of TNFα with its receptors. Infliximab does not neutralize TNFβ (lymphotoxin α), a related cytokine that utilizes the same receptors as TNFα. Biological activities attributed to TNFα include: induction of pro-inflammatory cytokines such as interleukins (IL) 1 and 6, enhancement of leukocyte migration by increasing endothelial layer permeability and expression of adhesion molecules by endothelial cells and leukocytes, activation of neutrophil and eosinophil functional activity, induction of acute phase reactants and other liver proteins, as well as tissue degrading enzymes produced by synoviocytes and/or chondrocytes. Cells expressing transmembrane TNFα bound by infliximab can be lysed in vitro or in vivo. Infliximab inhibits the functional activity of TNFα in a wide variety of in vitro bioassays utilizing human fibroblasts, endothelial cells, neutrophils, B and T lymphocytes and epithelial cells. The relationship of these biological response markers to the mechanism(s) by which REMICADE exerts its clinical effects is unknown. Anti-TNFα antibodies reduce disease activity in the cotton-top tamarin colitis model, and decrease synovitis and joint erosions in a murine model of collagen-induced arthritis. Infliximab prevents disease in transgenic mice that develop polyarthritis as a result of constitutive expression of human TNFα, and when administered after disease onset, allows eroded joints to heal. Dosing (Adults): Crohn's disease: Induction regimen: 5 mg/kg IV over 2 hours. Repeat dose at 2 and 6 weeks, followed by 5 mg/kg every 8 weeks. Dose may be increased to 10 mg/kg in patients who respond but then lose their response. If no response by week 14, consider discontinuing therapy. Psoriatic arthritis (with or without methotrexate): 5 mg/kg IV at 0, 2, and 6 weeks, then every 8 weeks. Rheumatoid arthritis: (In combination with methotrexate therapy): 3 mg/kg IV at 0, 2, and 6 weeks then every 8 weeks thereafter. Doses have ranged from 3-10 mg/kg intravenous infusion repeated at 4 to 8 week intervals. Dosage adjustment with CHF: Weigh risk versus benefits for individual patient: |
Mesalamine (asacol ®, pentasa ®)
| CLINICAL PHARMACOLOGY Mesalamine is thought to be the major therapeutically active part of the sulfasalazine molecule in the treatment of ulcerative colitis. Sulfasalazine is converted to equimolar amounts of sulfapyridine and mesalamine by bacterial action in the colon. The usual oral dose of sulfasalazine for active ulcerative colitis is 3 to 4 grams daily in divided doses, which provides 1.2 to 1.6 grams of mesalamine to the colon. The mechanism of action of mesalamine (and sulfasalazine) is unknown, but appears to be topical rather than systemic. Mucosal production of arachidonic acid (AA) metabolites, both through the cyclooxygenase pathways, i.e., prostanoids, and through the lipoxygenase pathways, i.e., leukotrienes (LTs) and hydroxyeicosatetraenoic acids (HETEs), is increased in patients with chronic inflammatory bowel disease, and it is possible that mesalamine diminishes inflammation by blocking cyclooxygenase and inhibiting prostaglandin (PG) production in the colon. Adults (usual course of therapy is 3-8 weeks): Maintenance of remission of ulcerative colitis: Rectal: Rectal suppository (Canasa™): Note: Suppositories should be retained for at least 1-3 hours to achieve maximum benefit. Elderly: See adult dosing; use with caution Administration Supplied SELECTED INDIVIDUAL PRODUCT MONOGRAPHS (Mesalamine)APRISO™ (mesalamine) extended-release capsules: DOSAGE AND ADMINISTRATION DOSAGE FORMS AND STRENGTHS -------------------- The suppository should be retained for one to three hours or longer, if possible, to achieve the maximum benefit. While the effect of CANASA® suppositories may be seen within three to twenty-one days, the usual course of therapy would be from three to six weeks depending on symptoms and sigmoidoscopic findings. Studies have suggested that CANASA® suppositories will delay relapse after the six-week short-term treatment. -------------------- DOSAGE AND ADMINISTRATION: DOSAGE FORMS AND STRENGTHS Asacol® For the maintenance of remission of ulcerative colitis: The recommended dosage in adults is 1.6 grams daily, in divided doses. Treatment duration in the prospective, well-controlled trial was 6 months. Two Asacol 400 mg tablets have not been shown to be bioequivalent to one Asacol HD 800 mg tablet. DOSAGE AND ADMINISTRATION Initial U.S. Approval: 2013 Mechanism of Action: The mechanism of action of mesalamine is unknown, but appears to be topical rather than systemic. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways, that is, prostanoids, and through the lipoxygenase pathways, that is, leukotrienes and hydroxyeicosatetraenoic acids, is increased in patients with chronic ulcerative colitis, and it is possible that mesalamine diminishes inflammation by blocking cyclooxygenase and inhibiting prostaglandin production in the colon. INDICATIONS AND USAGE: DELZICOL is an aminosalicylate indicated for: HOW SUPPLIED: Delayed-release capsules: 400 mg |
Olsalazine (dipentum ® )
| CLINICAL PHARMACOLOGY After oral administration, olsalazine has limited systemic bioavailability. Based on oral and intravenous dosing studies, approximately 2.4% of a single 1.0 g oral dose is absorbed. Less than 1% of olsalazine is recovered in the urine. The remaining 98 to 99% of an oral dose will reach the colon, where each molecule is rapidly converted into two molecules of 5-aminosalicylic acid (5-ASA) by colonic bacteria and the low prevailing redox potential found in this environment. The liberated 5-ASA is absorbed slowly resulting in very high local concentrations in the colon. The conversion of olsalazine to mesalamine (5-ASA) in the colon is similar to that of sulfasalazine, which is converted into sulfapyridine and mesalamine. It is thought that the mesalamine component is therapeutically active in ulcerative colitis (A.K. Azad-Kahn et al, LANCET, 2: 892-895, 1977). The usual dose of sulfasalazine for maintenance of remission in patients with ulcerative colitis is 2 grams daily, which would provide approximately 0.8 grams of mesalamine to the colon. More than 0.9 grams of mesalamine would usually be made available in the colon from 1 gram of olsalazine. The mechanism of action of mesalamine (and sulfasalazine) is unknown, but appears to be topical rather than systemic. Mucosal production of arachidonic acid (AA) metabolites, both through the cyclooxygenase pathways (i.e., prostanoids) and through the lipoxygenase pathways (i.e., leukotrienes [LTs] and hydroxyeicosatetraenoic acids [HETEs]) is increased in patients with chronic inflammatory bowel disease, and it is possible that mesalamine diminishes inflammation by blocking cyclooxygenase and inhibiting prostaglandin (PG) production in the colon. INDICATIONS AND USAGE CONTRAINDICATIONS Dosing (Adults): Ulcerative colitis: 500mg orally bid. Administration |
Sulfasalazine (azulfidine ®)
| CLINICAL PHARMACOLOGY Pharmacodynamics The mode of action of sulfasalazine (SSZ) or its metabolites, 5-aminosalicylic acid (5-ASA) and sulfapyridine (SP), is still under investigation, but may be related to the anti-inflammatory and/or immunomodulatory properties that have been observed in animal and in vitro models, to its affinity for connective tissue, and/or to the relatively high concentration it reaches in serous fluids, the liver and intestinal walls, as demonstrated in autoradiographic studies in animals. In ulcerative colitis, clinical studies utilizing rectal administration of SSZ, SP, and 5-ASA have indicated that the major therapeutic action may reside in the 5-ASA moiety. INDICATIONS AND USAGE a. in the treatment of mild to moderate ulcerative colitis, and as adjunctive therapy in severe ulcerative colitis; and CONTRAINDICATIONS Patients with intestinal or urinary obstruction, Adults: Rheumatoid arthritis: Enteric coated tablet: Initial: 0.5-1 g/day; increase weekly to maintenance dose of 2 g/day in 2 divided doses; maximum: 3 g/day (if response to 2 g/day is inadequate after 12 weeks of treatment) Dosing interval in renal impairment: Administration Supplied |
Vedolizumab- entyvio ® for injection
| Drug UPDATES: ENTYVIO (vedolizumab) for injection, for intravenous use [Drug information / PDF] Dosing: Click (+) next to Dosage and Administration section (drug info link) Initial U.S. Approval: 2014 Mechanism of Action: Vedolizumab is a humanized monoclonal antibody that specifically binds to the a4ß7 integrin and blocks the interaction of a4ß7 integrin with mucosal addressin cell adhesion molecule-1 (MAdCAM-1) and inhibits the migration of memory T-lymphocytes across the endothelium into inflamed gastrointestinal parenchymal tissue. Vedolizumab does not bind to or inhibit function of the a4ß1 and aEß7 integrins and does not antagonize the interaction of a4 integrins with vascular cell adhesion molecule-1 (VCAM-1). INDICATIONS AND USAGE: in adult patients with moderately to severely active ulcerative colitis who have had an inadequate response with, lost response to, or were intolerant to a tumor necrosis factor (TNF) blocker or immunomodulator; or had an inadequate response with, were intolerant to, or demonstrated dependence on corticosteroids. 1.2 Adult Crohn’s Disease -in adult patients with moderately to severely active Crohn’s disease who have had an inadequate response with, lost response to, or were intolerant to a tumor necrosis factor (TNF) blocker or immunomodulator; or had an inadequate response with, were intolerant to, or demonstrated dependence on corticosteroids. HOW SUPPLIED: ENTYVIO for injection: 300 mg of vedolizumab as a lyophilized cake in single dose 20 mL vials for reconstitution. |
Reference(s)
National Institutes of Health, U.S. National Library of Medicine, DailyMed Database.
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