Olsalazine

Upon reaching the colon, colonic bacteria convert olsalazine into 5‑aminosalicylic acid (5-ASA or mesalazine). The mechanism of action of 5-ASA (mesalamine) is not fully understood, but appears to be a topical anti-inflammatory effect on colonic epithelial cells.

• DIPENTUM is indicated for the maintenance of remission of ulcerative colitis in adult patients who are intolerant of sulfasalazine. DIPENTUM is an aminosalicylate indicated for the maintenance of remission of ulcerative colitis in adult patients who are intolerant of sulfasalazine.ICD-10: K51.90

• DIPENTUM is contraindicated in patients with known or suspected hypersensitivity to salicylates, aminosalicylates, or to any of the excipients in DIPENTUM [see Warnings and Precautions (5.3) , Description (11) ] . Known or suspected hypersensitivity to salicylates or aminosalicylates or to any of the ingredients of DIPENTUM.contraindicated

Evaluate renal function before initiating therapy with DIPENTUM [see Warnings and Precautions (5.1) ]. The recommended dosage is 500 mg orally twice daily. Drink an adequate amount of fluids during treatment [see Warnings and Precautions (5.7) ] . • Evaluate renal function prior to initiation of DIPENTUM and periodically while on therapy. ( 2 , 5.1 ) • The recommended dosage is 500 mg orally twice daily. ( 2 ) • Drink an adequate amount of fluids. ( 2 , 5.7 )

• Renal Impairment : Assess renal function at the beginning of treatment and periodically during treatment. Discontinue DIPENTUM if renal function deteriorates while on therapy. ( 5.1 , 7.1 ) • Mesalamine-Induced Acute Intolerance Syndrome : Discontinue treatment if acute intolerance syndrome (cramping, acute abdominal pain, bloody diarrhea, sometimes fever, headache and rash) is suspected. ( 5.2 ) • Hypersensitivity Reactions, including myocarditis and pericarditis : Discontinue DIPENTUM if a hypersensitivity reaction is suspected. ( 5.3 ) • Hepatic Failure : Evaluate the risks and benefits of using DIPENTUM in patients with known liver impairment. ( 5.4 ) • Severe Cutaneous Adverse Reactions : Discontinue at the first signs or symptoms of severe cutaneous adverse reactions or other signs of hypersensitivity and consider further evaluation. ( 5.5 ) • Photosensitivity : Avoid sun exposure if pre-existing skin conditions. ( 5.6 ) • Nephrolithiasis : Cases of nephrolithiasis have been reported with the use of mesalamine. Mesalamine-containing stones are undetectable by standard radiography or computed tomography (CT). Ensure adequate hydration during treatment. ( 5.7 ) • Interference with Laboratory Tests : Mesalamine may lead to elevated urinary normetanephrine test results. ( 5.8 ) 5.1 Renal Impairment Renal impairment, including minimal change disease, acute and chronic interstitial nephritis, and renal failure have been reported in patients given DIPENTUM or other products that contain mesalamine or are converted to mesalamine.

The following clinically significant adverse reactions are described elsewhere in the labeling: • Renal impairment [see Warnings and Precautions (5.1) ] • Mesalamine-induced acute intolerance syndrome [see Warnings and Precautions (5.2) ] • Hypersensitivity reactions [see Warnings and Precautions (5.3) ] • Hepatic failure [see Warnings and Precautions (5.4) ] • Severe cutaneous adverse reactions [see Warnings and Precautions (5.5) ] • Photosensitivity [see Warnings and Precautions (5.6) ] • Nephrolithiasis [see Warnings and Precautions (5.7) ] The following adverse reactions have been identified from clinical studies or postmarketing reports of olsalazine. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. In double-blind, placebo- and active-controlled clinical trials of ulcerative colitis, discontinuations due to adverse reactions were reported in 10% of DIPENTUM-treated patients (N=441) and 7% of placebo-treated patients (N=208). Both sulfasalazine-tolerant and intolerant patients were included. The most common adverse reactions leading to discontinuation in DIPENTUM-treated patients were diarrhea/loose stools (6%), abdominal pain (1%), and rash/itching (1%). In these controlled trials, adverse reactions reported in 1% or more of patients treated with DIPENTUM and greater than placebo are provided in Table 1.

Geriatric Patients : Increased risk of blood dyscrasias; monitor complete blood cell counts and platelet counts. ( 8.5 ) 8.1 Pregnancy Risk Summary Published data from meta-analyses, cohort studies and case series on the use of mesalamine, the active moiety in DIPENTUM, during pregnancy have not reliably informed an association with mesalamine and major birth defects, miscarriage, or adverse maternal or fetal outcomes (see Data ) . There are adverse effects on maternal and fetal outcomes associated with ulcerative colitis in pregnancy (see Clinical Considerations ) . In animal reproduction studies, there were adverse developmental effects observed after oral administration of olsalazine sodium in pregnant rats during organogenesis at doses of 5 to 20 times the maximum recommended human dose (see Data ) . The background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.

Metabolism

Olsalazine The usual dose of sulfasalazine for maintenance of remission in patients with ulcerative colitis is 2 grams daily, which would provide approximately 0.8 gram of mesalamine to the colon. More than 0.9 gram of mesalamine would usually be made available in the colon from 1 gram of olsalazine.

DIPENTUM is an aminosalicylate, and symptoms of salicylate toxicity include: nausea, vomiting and abdominal pain, tachypnea, hyperpnea, tinnitus, and neurologic symptoms (headache, dizziness, confusion, seizures). Severe salicylate intoxication may lead to electrolyte and blood pH imbalance and potentially to other organ (e.g., renal and liver) damage. There is no specific antidote for olsalazine overdose; however, conventional therapy for salicylate toxicity may be beneficial in the event of acute overdosage and may include gastrointestinal tract decontamination to prevent of further absorption. Correct fluid and electrolyte imbalance by the administration of appropriate intravenous therapy and maintain adequate renal function.

• Jul 31, 1990NDANDA019715Mylan Spclt Viatris

1. 1Colitis Ulcerative199.7%
2. 2Diarrhoea147.1%
3. 3Drug Ineffective126.1%
4. 4Off Label Use115.6%
5. 5Fatigue94.6%
6. 6Pain84.1%
7. 7Pain In Extremity73.6%
8. 8Pruritus73.6%
9. 9Pyrexia73.6%
10. 10Anxiety63.1%
11. 11Arthralgia63.1%
12. 12Chest Pain63.1%
13. 13Haematochezia63.1%
14. 14Malaise63.1%
15. 15Nausea63.1%

The 2 most recently updated of 2 ClinicalTrials.gov registrations naming Olsalazine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Randomized Placebo-Controlled Trial of Budesonide Multi-Matrix System (MMX®) 9 Milligrams (mg) in Participants With Ulcerative Colitis Currently on a 5-Aminosalicylic Acid (5-ASA)
  Completed · Phase 3 · Interventional · 510 enrolled · Bausch Health Americas, Inc.
  NCT01532648updated 2019-09-06
• Phase II Pilot Study of Olsalazine for Ankylosing Spondylitis
  Completed · Phase 2 · Interventional · 4 enrolled · National Center for Research Resources (NCRR)
  NCT00004288updated 2005-06-24

Frequently asked questions

How does Olsalazine work?

Upon reaching the colon, colonic bacteria convert olsalazine into 5‑aminosalicylic acid (5-ASA or mesalazine). The mechanism of action of 5-ASA (mesalamine) is not fully understood, but appears to be a topical anti-inflammatory effect on colonic epithelial cells.

What is Olsalazine used for?

According to FDA labeling, Olsalazine carries indications including: DIPENTUM is indicated for the maintenance of remission of ulcerative colitis in adult patients who are intolerant of sulfasalazine. DIPENTUM is an aminosalicylate indicated for the maintenance of remission of ulcerative colitis in adult patients who are intolerant of sulfasalazine.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Olsalazine?

Olsalazine is classified as Aminosalicylic acid and similar agents, Aminosalicylate, Cyclooxygenase Inhibitors, Lipoxygenase Inhibitors, Decreased Platelet Aggregation, Decreased Prostaglandin Production, Decreased Thromboxane Production.

What are the brand names for Olsalazine?

Olsalazine is marketed under brand names including Dipentum.

What are the contraindications for Olsalazine?

Olsalazine labeling lists contraindications including: DIPENTUM is contraindicated in patients with known or suspected hypersensitivity to salicylates, aminosalicylates, or to any of the excipients in DIPENTUM [see Warnings and Precautions (5.3) , Description (11) ] . Known or suspected hypersensitivity to salicylates or aminosalicylates or to any of the ingredients of DIPENTUM.. Always consult the full prescribing information and a clinician.