Version May 2024
Ulcerative colitis, mildly to moderately active (alternative agent):
Note: For use as an alternative to other preferred therapies; olsalazine is frequently not tolerated due to drug-induced diarrhea (Ref).
Remission induction (off-label use): Oral: 2 to 3 g/day in 2 to 4 divided doses (Ref).
Maintenance of remission: Oral: 1 g/day in 2 divided doses.
There are no dosage adjustments provided in the manufacturer's labeling; almost all of 5-ASA in the urine is found as the inactive acetylated metabolite. However, due to reports of kidney impairment related to the use of mesalamine-containing products, evaluate risk versus benefit before starting therapy in patients with preexisting impairment, with history of kidney disease, or taking concomitant nephrotoxic medications. If necessary, use with caution and close monitoring of kidney function.
Kidney impairment during treatment: Discontinue use if kidney function deteriorates during treatment.
There are no dosage adjustments provided in the manufacturer's labeling; evaluate risk versus benefit in patients with preexisting impairment.
Refer to adult dosing.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported in adults.
>10%: Gastrointestinal: Diarrhea (11% to 17%)
1% to 10%:
Dermatologic: Pruritus (1%), skin rash (2%)
Gastrointestinal: Abdominal cramps (≤10%), abdominal pain (≤10%), bloating (2%), nausea (5%), stomatitis (1%), vomiting (1%)
Nervous system: Depression (2%), dizziness (≤1%), vertigo (≤1%)
Neuromuscular & skeletal: Arthralgia (4%)
Respiratory: Upper respiratory tract infection (2%)
<1%:
Cardiovascular: Chest pain, hypertension, myocarditis, orthostatic hypotension, palpitations, pericarditis, peripheral edema, second degree atrioventricular block, tachycardia
Dermatologic: Alopecia, erythema nodosum, erythema of skin, skin photosensitivity
Endocrine & metabolic: Dehydration, heavy menstrual bleeding, hot flash
Gastrointestinal: Blood in stool, epigastric discomfort, flatulence, pancreatitis, rectal irritation (discomfort), xerostomia
Genitourinary: Dysuria, hematuria, impotence, nephrotic syndrome, proteinuria, urinary frequency
Hematologic & oncologic: Anemia, eosinophilia, hemolytic anemia, leukopenia, lymphocytopenia, neutropenia, rectal hemorrhage, reticulocytosis, thrombocytopenia
Hepatic: Cholestatic hepatitis, granulomatous hepatitis, hepatitis, increased serum alanine aminotransferase, increased serum aspartate aminotransferase
Nervous system: Chills, emotional lability, insomnia, irritability, paresthesia, rigors
Neuromuscular & skeletal: Muscle cramps, tremor
Ophthalmic: Blurred vision, watery eyes, xerophthalmia
Otic: Tinnitus
Renal: Interstitial nephritis
Respiratory: Bronchospasm, dyspnea, interstitial pulmonary disease
Miscellaneous: Fever
Postmarketing:
Dermatologic: Acute generalized exanthematous pustulosis, Stevens-Johnson syndrome, toxic epidermal necrolysis
Endocrine & metabolic: Increased gamma-glutamyl transferase, increased lactate dehydrogenase, Kawasaki-like syndrome
Hematologic & oncologic: Aplastic anemia, pancytopenia
Hepatic: Cholestatic jaundice, hepatic cirrhosis, hepatic failure, hepatic necrosis, increased serum alkaline phosphatase, increased serum bilirubin, jaundice
Hypersensitivity: Angioedema
Immunologic: Drug reaction with eosinophilia and systemic symptoms
Nervous system: Peripheral neuropathy
Neuromuscular & skeletal: Myalgia
Renal: Nephrolithiasis, renal failure syndrome, renal insufficiency
Respiratory: Pleurisy
Hypersensitivity to olsalazine, aminosalicylates, salicylates, or metabolites or any component of the formulation
Concerns related to adverse effects:
• Dermatologic reactions: Severe cutaneous adverse reactions, including acute generalized exanthematous pustulosis, drug reaction with eosinophilia and systemic symptoms, Stevens-Johnson syndrome, and toxic epidermal necrolysis, have been reported. If a reaction occurs, discontinue immediately and consider further evaluation.
• Diarrhea: Commonly occurs and may be dose related; must be distinguished from underlying symptoms of ulcerative colitis.
• Hypersensitivity reactions: Mesalamine-induced hypersensitivity reactions have been reported and may include internal organ involvement, such as hepatitis, myocarditis, pericarditis, nephritis, hematologic abnormalities, and/or pneumonitis. Monitor for signs and symptoms of hypersensitivity; discontinue treatment if hypersensitivity occurs.
• Intolerance syndrome: May cause an acute intolerance syndrome (cramping, acute abdominal pain, bloody diarrhea; sometimes fever, headache, rash); may be hard to discern from an exacerbation; monitor for worsening of symptoms and discontinue immediately if syndrome occurs or is suspected.
• Photosensitivity: Use with caution in patients with preexisting skin conditions (including atopic dermatitis and atopic eczema); severe photosensitivity reactions have been reported. Use skin protection (protective clothing and broad-spectrum sunscreen) and avoid prolonged exposure to sunlight and ultraviolet light.
• Renal effects: Renal impairment (including minimal change disease, acute and chronic interstitial nephritis, and renal failure) has been reported. A renal function evaluation is recommended prior to initiation of therapy and periodically during treatment. Evaluate risk versus benefit in patients with renal impairment, with a history of renal disease, or concurrently taking nephrotoxic medications. Cases of nephrolithiasis (including stones with 100% mesalamine content) have occurred with mesalamine use. Stones may be radiotransparent and undetectable by standard imaging. Ensure patients are adequately hydrated during therapy.
• Sulfasalazine hypersensitivity: Patients with hypersensitivity to sulfasalazine may react to mesalamine.
Disease-related concerns:
• Hepatic impairment: Evaluate risk versus benefit if therapy in patients with hepatic impairment; hepatic failure has been observed with other mesalamine (5-aminosalicylic acid) products.
• Renal impairment: Use with caution in patients with renal impairment, with a history of renal disease, or on nephrotoxic medications.
Special populations:
• Older adult: Use with caution in patients ≥65 years of age; uncontrolled studies and postmarketing reports suggest an increased incidence of blood dyscrasias (ie, agranulocytosis, neutropenia, pancytopenia) in patients ≥65 years of age taking mesalamine-containing products.
Other warnings/precautions:
• Urine discoloration: Urine may appear reddish-brown when it comes in contact with surfaces or water (eg, in toilet) treated with hypochlorite-containing bleach; if discoloration occurs, instruct patients to observe urine flow as it leaves the body and contact health care provider if discoloration is seen prior to contact with any surface or water.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, Oral, as sodium:
Dipentum: 250 mg
No
Capsules (Dipentum Oral)
250 mg (per each): $17.06
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, Oral, as sodium:
Dipentum: 250 mg
Oral: Administer with food in evenly divided doses. Maintain adequate hydration during therapy (to minimize nephrolithiasis risk).
Ulcerative colitis, mildly to moderately active, maintenance of remission: Maintenance of remission of ulcerative colitis in adults intolerant to sulfasalazine.
Limitations of use: Based on the American Gastroenterological Association (AGA) guidelines on the management of moderate to severe ulcerative colitis, if remission is achieved with concomitant biologic agents or immunomodulators, olsalazine should not be continued for maintenance of remission (AGA [Feuerstein 2020]).
Ulcerative colitis, mildly to moderately active, remission induction
Olsalazine may be confused with OLANZapine.
Dipentum may be confused with Dilantin.
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Cardiac Glycosides: 5-Aminosalicylic Acid Derivatives may decrease the serum concentration of Cardiac Glycosides. Risk C: Monitor therapy
Myelosuppressive Agents: 5-Aminosalicylic Acid Derivatives may enhance the myelosuppressive effect of Myelosuppressive Agents. Risk C: Monitor therapy
Nonsteroidal Anti-Inflammatory Agents: May enhance the nephrotoxic effect of 5-Aminosalicylic Acid Derivatives. Risk C: Monitor therapy
Thiopurine Analogs: 5-Aminosalicylic Acid Derivatives may enhance the myelosuppressive effect of Thiopurine Analogs. 5-Aminosalicylic Acid Derivatives may increase serum concentrations of the active metabolite(s) of Thiopurine Analogs. Specifically, exposure to the active 6-thioguanine nucleotides (6-TGN) may be increased. Risk C: Monitor therapy
Varicella Virus-Containing Vaccines: 5-Aminosalicylic Acid Derivatives may enhance the adverse/toxic effect of Varicella Virus-Containing Vaccines. The primary concern is the potential development of Reye's Syndrome, a condition that has been associated with the use of salicylates in children with varicella infections. Management: Avoid administration of salicylates for at least 6 weeks after adminstration of a varicella virus-containing vaccine. Risk D: Consider therapy modification
Vitamin K Antagonists (eg, warfarin): 5-Aminosalicylic Acid Derivatives may enhance the anticoagulant effect of Vitamin K Antagonists. 5-Aminosalicylic Acid Derivatives may diminish the anticoagulant effect of Vitamin K Antagonists. Risk C: Monitor therapy
Animal studies have demonstrated fetal developmental toxicities. There are no well-controlled studies in pregnant women. Use during pregnancy only if clearly necessary.
The active metabolite, 5-aminosalicylic acid may pass into breast milk. Diarrhea has been reported in breastfed infants whose mothers took olsalazine.
Renal function (prior to and periodically during therapy); CBC (particularly in patients ≥65 years of age); hepatic function; signs/symptoms of worsening acute intolerance syndrome, dermatologic toxicity, or hypersensitivity reactions.
Mesalamine (5-aminosalicylic acid) is the active component of olsalazine; 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, and is also postulated to be a free radical scavenger or an inhibitor of tumor necrosis factor (TNF); action appears topical rather than systemic.
Absorption: <3%; very little intact olsalazine is systemically absorbed
Protein binding, plasma: >99%
Metabolism: Primarily via colonic bacteria to active drug, 5-aminosalicylic acid (5-ASA)
Half-life elimination: 54 minutes
Time to peak: ~1 hour
Excretion: Primarily feces; urine (<1%)
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