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BROWSE topics
Inflammatory bowel disease - Common medications
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balsalazide (Colazal ® )
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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] |
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budesonide (Entocort EC ®,
UCERIS® )
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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 INDICATIONS: UCERIS (budesonide) is a glucocorticosteroid indicated for the induction of remission in patients with active, mild to moderate ulcerative colitis. DOSAGE AND ADMINISTRATION ENTOCORT EC Usual dose ( adults): 9 mg taken once daily in the morning for up to 8 weeks. Safety and efficacy have not been established beyond 8 weeks. For recurring episodes of active Crohn's Disease, a repeat 8 week course of Entocort EC ® can be given. Treatment can be tapered to 6 mg daily for 2 weeks prior to complete cessation. Patients with mild to moderate active Crohn's disease have been switched from oral prednisolone to Entocort EC ® with no reported episodes of adrenal insufficiency. Since prednisolone should not be stopped abruptly, tapering should begin concomitantly with initiating Entocort EC ® treatment. UCERIS® The recommended dosage for the induction of remission in adult patients with active, mild to moderate ulcerative colitis is one 9 mg tablet to be taken once daily in the morning with or without food for up to 8 weeks. DOSAGE FORMS AND STRENGTHS: Capsule: 3 mg capsule, ENTOCORT EC. Tablet: extended release tablets: 9 mg UCERIS® |
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infliximab (Remicade ®)
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CLINICAL PHARMACOLOGY General Infliximab neutralizes the biological activity of TNF  by binding with
high affinity to the soluble and transmembrane forms of TNF and
inhibits binding of TNF with its receptors. Infliximab does not
neutralize TNF (lymphotoxin ), a related cytokine that utilizes the
same receptors as TNF. Biological activities attributed to TNF
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 TNF
bound by infliximab can be lysed in vitro or in vivo. Infliximab
inhibits the functional activity of TNF 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-TNF 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 TNF, and
when administered after disease onset, allows eroded joints to heal.Dosing (Adults): Ankylosing spondylitis: 5 mg/kg IV at 0, 2, and 6 weeks, followed by 5 mg/kg every 6 weeks thereafter. 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: NYHA Class III or IV: </=5 mg/kg |
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mesalamine (Asacol ®, Pentasa ®)
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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): Oral: Treatment of ulcerative colitis: Capsule: 1 g 4 times/day Tablet: Initial: 800 mg (2 tablets) 3 times/day for 6 weeks Maintenance of remission of ulcerative colitis: Capsule: 1 g 4 times/day Tablet: 1.6 g/day in divided doses Rectal: Retention enema: 60 mL (4 g) at bedtime, retained overnight, approximately 8 hours Rectal suppository (Canasa™): 500 mg: Insert 1 suppository in rectum twice daily; may increase to 3 times/day if inadequate response is seen after 2 weeks. 1000 mg: Insert 1 suppository in rectum daily at bedtime Note: Suppositories should be retained for at least 1-3 hours to achieve maximum benefit. Note: Some patients may require rectal and oral therapy concurrently. Elderly: See adult dosing; use with caution Administration Oral: Swallow capsules or tablets whole, do not chew or crush. Rectal enema: Shake bottle well. Retain enemas for 8 hours or as long as practical. Suppository: Remove foil wrapper; avoid excessive handling. Should be retained for at least 1-3 hours to achieve maximum benefit. Supplied Capsule, controlled release (Pentasa®): 250 mg Extended-release capsules: 0.375 g APRISO™ Suppository, rectal (Canasa™): 500 mg, 1000 mg [contains saturated vegetable fatty acid esters] Suspension, rectal: 4 g/60 mL (7s) [contains potassium metabisulfite and sodium benzoate] Rowasa®: 4 g/60 mL (7s, 28s) [contains potassium metabisulfite and sodium benzoate] Tablet, delayed release [enteric coated] (Asacol®): 400 mg Asacol® HD -800 mg delayed-release tablet SELECTED INDIVIDUAL PRODUCT MONOGRAPHS (Mesalamine)APRISO™ (mesalamine) extended-release capsules: APRISO is a locally-acting aminosalicylate indicated for the maintenance of remission of ulcerative colitis in adults. DOSAGE AND ADMINISTRATION Four APRISO capsules once daily (1.5 g/day) in the morning with or without food. Do not co-administer with antacids. DOSAGE FORMS AND STRENGTHS Extended-release capsules: 0.375 g -------------------- CANASA® (mesalamine, USP) 1000 mg suppositories DOSAGE AND ADMINISTRATION The usual dosage of CANASA® (mesalamine, USP) 1000 mg suppositories is one rectal suppository 1 time daily at bedtime. 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. -------------------- LIALDA® is a locally acting 5-aminosalicylic acid (5-ASA) indicated for the induction of remission in adults with active, mild to moderate ulcerative colitis and for the maintenance of remission of ulcerative colitis. DOSAGE AND ADMINISTRATION: For induction of remission of active, mild to moderate ulcerative colitis, two to four 1.2 g tablets taken once daily with food. For maintenance of remission of ulcerative colitis, two 1.2 g tablets taken once daily with food. (1, 2) DOSAGE FORMS AND STRENGTHS Delayed-Release Tablets: 1.2 g ------------------------ Asacol® DOSAGE AND ADMINISTRATION For the treatment of mildly to moderately active ulcerative colitis: The usual dosage in adults is two 400-mg tablets to be taken three times a day for a total daily dose of 2.4 grams for a duration of 6 weeks. 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. ------------------------ Asacol® HD (mesalamine) delayed-release tablet for oral administration DOSAGE AND ADMINISTRATION Two 800 mg tablets three times daily for 6 weeks. Asacol HD should be swallowed whole without cutting, breaking, or chewing. One Asacol HD 800 mg tablet has not been shown to be bioequivalent to two Asacol® (mesalamine) delayed-release 400 mg tablets. |
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olsalazine (Dipentum ® )
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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 Olsalazine is indicated for the maintenance of remission of ulcerative colitis in patients who are intolerant of sulfasalazine. CONTRAINDICATIONS Hypersensitivity to olsalazine, other salicylates, or any of the excipients. Dosing (Adults): Ulcerative colitis: 500mg orally bid. Administration Take with food in evenly divided doses. Supplied Capsule, as sodium: 250 mg |
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sulfasalazine (Azulfidine ®)
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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 Sulfasalazine tablets are indicated: a. in the treatment of mild to moderate ulcerative colitis, and as adjunctive therapy in severe ulcerative colitis; and b. for the prolongation of the remission period between acute attacks of ulcerative colitis. CONTRAINDICATIONS Sulfasalazine tablets are contraindicated in: Patients with intestinal or urinary obstruction, Patients with porphyria, Patients hypersensitive to sulfasalazine, its metabolites, sulfonamides or salicylates Adults: Ulcerative colitis: Initial: 1 g 3-4 times/day, 2 g/day maintenance in divided doses; may initiate therapy with 0.5-1 g/day 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: Clcr 10-30 mL/minute: Administer twice daily Clcr<10 mL/minute: Administer once daily Dosing adjustment in hepatic impairment: Avoid use Administration GI intolerance is common during the first few days of therapy (administer with meals). Supplied Tablet (Azulfidine®): 500 mg Tablet, delayed release, enteric coated (Azulfidine® EN-tabs®): 500 mg |
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