Inflammatory bowel disease - Common medications

balsalazide (Colazal ® ) budesonide (Entocort EC ® )
infliximab (Remicade ®) mesalamine (Asacol®, Pentasa®)
olsalazine (Dipentum ® ) sulfasalazine (Azulfidine ®)

balsalazide (Colazal ® )  top of page icon

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]

budesonide (Entocort EC ® )  top of page icon

Indication: treatment of mild to moderate active Crohn's disease involving the ileum and/or the ascending colon. Budesonide has a high topical glucocorticosteroid (GCS) activity and a substantial first pass elimination.
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.

[Supplied: 3 mg capsule]

infliximab (Remicade ®)  top of page icon

 Monoclonal antibody to tumor necrosis factor.
INDICATIONS
Ankylosing spondylitis: Improving signs and symptoms of disease

Crohn's disease: Induction and maintenance of remission in patients with moderate to severe disease who have an inadequate response to conventional therapy; to reduce the number of draining enterocutaneous and rectovaginal fistulas and to maintain fistula closure

Rheumatoid arthritis: Inhibits the progression of structural damage and improves physical function in patients with moderate to severe disease; used with methotrexate

Mechanism of Action
Infliximab is a chimeric monoclonal antibody that binds to human tumor necrosis factor alpha (TNF-alpha), thereby interfering with endogenous TNF-alpha activity. Biological activities of TNF-alpha include the induction of pro-inflammatory cytokines (interleukins), enhancement of leukocyte migration, activation of neutrophils and eosinophils, and the induction of acute phase reactants and tissue degrading enzymes. Animal models have shown TNF-alpha expression causes polyarthritis, and infliximab can prevent disease as well as allow diseased joints to heal. Monoclonal antibody that binds to tumor necrosis factor. Biological activities of TNFa include the induction of proinflammatory cytokines (interleukins), enhancement of leukocyte migration, activation of neutrophils and eosinophils, and the induction of acute phase reactants and tissue degrading enzymes.

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

mesalamine (Asacol ®, Pentasa ®)   top of page icon

INDICATIONS
Oral: Treatment and maintenance of remission of mildly to moderately active ulcerative colitis
Rectal: Treatment of active mild to moderate distal ulcerative colitis, proctosigmoiditis, or proctitis

Mechanism of Action
Mesalamine (5-aminosalicylic acid) is the active component of sulfasalazine; the specific mechanism of action of mesalamine is unknown; however, it is thought that it modulates local chemical mediators of the inflammatory response, especially leukotrienes; action appears topical rather than systemic

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
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

olsalazine (Dipentum ® )  top of page icon

INDICATIONS
Maintenance of remission of ulcerative colitis in patients intolerant to sulfasalazine

Dosing (Adults): Ulcerative colitis: 500mg orally bid.

Administration
Take with food in evenly divided doses.
Supplied
Capsule, as sodium: 250 mg

sulfasalazine (Azulfidine ®)  top of page icon

INDICATIONS
Management of ulcerative colitis; enteric coated tablets are also used for rheumatoid arthritis (including juvenile rheumatoid arthritis) in patients who inadequately respond to analgesics and NSAIDs

Mechanism of Action
Acts locally in the colon to decrease the inflammatory response and systemically interferes with secretion by inhibiting prostaglandin synthesis

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
 

Disclaimer

Listed dosages are for - Adult patients ONLY. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER. GlobalRPH does not directly or indirectly practice medicine or provide medical services and therefore assumes no liability whatsoever of any kind for the information and data accessed through the Service or for any diagnosis or treatment made in reliance thereon.

David F. McAuley, Pharm.D., R.Ph.  GlobalRPh Inc.