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Inflammatory bowel disease - Common medications

balsalazide (Colazal ® ) balsalazide disodium - GIAZO®
budesonide (Entocort EC®, UCERIS® ) infliximab (Remicade ®)
mesalamine (Asacol®, DELZICOL ® Pentasa®) olsalazine (Dipentum ® )
sulfasalazine (Azulfidine ®) vedolizumab- ENTYVIO ® for injection
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balsalazide (Colazal ® )  top of page

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®  top of page

Drug UPDATESGIAZO (balsalazide disodium) tablets, for oral use
[Drug information  /  PDF]  
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
GIAZO is a locally acting aminosalicylate indicated for the treatment of mildly to moderately active ulcerative colitis in male patients 18 years of age and older. (1)

Limitations of Use
Effectiveness in female patients was not demonstrated in clinical trials. (1)
SSafety and effectiveness of GIAZO beyond 8 weeks have not been established. (1)

DOSAGE AND ADMINISTRATION
Three 1.1 g GIAZOtablets 2 times a day (6.6 g/day) with or without food for up to 8 weeks.
DOSAGE FORMS AND STRENGTHS
Tablets: 1.1 g

CONTRAINDICATIONS
Patients with hypersensitivity to salicylates or to any of the components of GIAZO tablets or balsalazide metabolites.
WARNINGS AND PRECAUTIONS
Exacerbation of the symptoms of ulcerative colitis was reported. Observe patients closely for worsening of these symptoms while on treatment. (5.1)
RRenal impairment may occur. Assess renal function at the beginning of treatment and periodically during treatment. (5.2)
Use with caution with pre-existing liver disease. (5.3)

budesonide (Entocort EC ®, UCERIS® )  top of page

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®

------------------------New Product:---------------------------------------------------


DrugUCERIS® (budesonide) rectal foam
Initial U.S. Approval: 1997
[Drug information  /  PDF]  
Dosing:  Click (+) next to Dosage and Administration section (drug info link)

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
2.1 Dosage
The recommended dosage regimen is 1 metered dose administered rectally twice daily for 2 weeks followed by 1 metered dose administered rectally once daily for 4 weeks.

2.2 Administration Instructions
Advise patients:
UCERIS rectal foam is only to be applied rectally. It is not for oral use.
Before using UCERIS rectal foam, use the bathroom to empty your bowels.
Each applicator is coated with a lubricant. If additional lubrication is needed, petrolatum or petroleum jelly can also be used.
Warm the canister in the hands while shaking it vigorously for 10 to 15 seconds prior to use.
UCERIS rectal foam can be used in a standing, lying or sitting position (e.g., while using the toilet).
Apply UCERIS rectal foam in the morning and the evening for the first 2 weeks of treatment; then once daily in the evening for the next 4 weeks. When applied in the evening, use immediately prior to bedtime. Try not to empty your bowels again until the next morning.
Avoid concomitant use of CYP3A4 inhibitors (e.g., ketoconazole, grapefruit juice) during treatment with UCERIS rectal foam.


HOW SUPPLIED: UCERIS rectal foam contains 2 mg budesonide per metered dose.





infliximab (Remicade ®)  top of page

CLINICAL PHARMACOLOGY
General
Infliximab neutralizes the biological activity of TNFalpha by binding with high affinity to the soluble and transmembrane forms of TNFalpha and inhibits binding of TNFalpha with its receptors. Infliximab does not neutralize TNFbeta (lymphotoxin alpha), a related cytokine that utilizes the same receptors as TNFalpha. Biological activities attributed to TNFalpha 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 TNFalpha bound by infliximab can be lysed in vitro or in vivo. Infliximab inhibits the functional activity of TNFalpha 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-TNFalpha 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 TNFalpha, 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

mesalamine (Asacol ®, Pentasa ®)   top of page

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.
-------------------------
DELZICOL ® (mesalamine) delayed-release capsules, for oral use
[Drug information  /  PDF]  
Dosing:  Click (+) next to Dosage and Administration section (drug info link)

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:
Treatment of mildly to moderately active ulcerative colitis in patients 12 years of age and older (1.1)
Maintenance of remission of ulcerative colitis in adults

HOW SUPPLIED: Delayed-release capsules: 400 mg

olsalazine (Dipentum ® )  top of page

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

sulfasalazine (Azulfidine ®)  top of page

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

vedolizumab- ENTYVIO ® for injection  top of page

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 α4β7 integrin and blocks the interaction of α4β7 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 α4β1 and αEβ7 integrins and does not antagonize the interaction of α4 integrins with vascular cell adhesion molecule-1 (VCAM-1).
The α4β7 integrin is expressed on the surface of a discrete subset of memory T-lymphocytes that preferentially migrate into the gastrointestinal tract. MAdCAM-1 is mainly expressed on gut endothelial cells and plays a critical role in the homing of T-lymphocytes to gut lymph tissue. The interaction of the α4β7 integrin with MAdCAM-1 has been implicated as an important contributor to the chronic inflammation that is a hallmark of ulcerative colitis and Crohn’s disease.

INDICATIONS AND USAGE:
1.1 Adult Ulcerative Colitis
ENTYVIO (vedolizumab) is indicated for:
-inducing and maintaining clinical response,
-inducing and maintaining clinical remission,
-improving the endoscopic appearance of the mucosa, and
-achieving corticosteroid-free remission

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
ENTYVIO (vedolizumab) is indicated for:
-achieving clinical response,
-achieving clinical remission, and
-achieving corticosteroid-free remission

-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.
Provides access to the latest drug monographs submitted to the Food and Drug Administration (FDA). Please review the latest applicable package insert for additional information and possible updates.  A local search option of this data can be found here.

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.
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