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Olsalazine

Generic name: olsalazine systemic

Brand names: Dipentum

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule, Oral, as sodium:

Dipentum: 250 mg

Pharmacology

Mechanism of Action

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.

Pharmacokinetics/Pharmacodynamics

Absorption

<3%; very little intact olsalazine is systemically absorbed

Metabolism

Primarily via colonic bacteria to active drug, 5-aminosalicylic acid (5-ASA)

Excretion

Primarily feces; urine (<1%)

Time to Peak

~1 hour

Half-Life Elimination

54 minutes

Protein Binding

Plasma: >99%

Use: Labeled Indications

Ulcerative colitis, remission maintenance: Maintenance of remission of ulcerative colitis in patients intolerant to sulfasalazine.

Use: Off Label

Ulcerative colitis, remission inductionbyes

Data from 2 small randomized, double-blind, placebo-controlled studies and 1 small randomized study of olsalazine in the treatment of ulcerative colitis supports the use of olsalazine for induction of remission in patients with mild to moderate ulcerative colitis Feurle 1989, Kruis 1998, Zinberg 1990.

Based on the American Gastroenterological Association (AGA) guidelines on the management of mild to moderate ulcerative colitis, olsalazine is an option for induction of remission in patients with mild to moderate ulcerative colitis AGA [Ko 2019].

Contraindications

Hypersensitivity to olsalazine, salicylates, or any component of the formulation

Dosage and Administration

Dosing: Adult

Ulcerative colitis, remission maintenance: Oral: 1 g/day in 2 divided doses.

Ulcerative colitis, remission induction (off-label use): Oral: 2 to 3 g/day in 2 to 4 divided doses (Fuerle 1989; Kruis 1998; Zinberg 1990).

Dosing: Geriatric

Refer to adult dosing.

Administration

Oral: Administer with food in evenly divided doses.

Storage

Store at 20°C to 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).

Drug Interactions

Cardiac Glycosides: 5-Aminosalicylic Acid Derivatives may decrease the serum concentration of Cardiac Glycosides. Monitor therapy

Heparin: 5-Aminosalicylic Acid Derivatives may enhance the adverse/toxic effect of Heparin. Specifically, the risk for bleeding/bruising may be increased. Monitor therapy

Heparins (Low Molecular Weight): 5-Aminosalicylic Acid Derivatives may enhance the adverse/toxic effect of Heparins (Low Molecular Weight). Specifically, the risk for bleeding/bruising may be increased. Monitor therapy

Nonsteroidal Anti-Inflammatory Agents: May enhance the nephrotoxic effect of 5-Aminosalicylic Acid Derivatives. Monitor therapy

Thiopurine Analogs: 5-Aminosalicylic Acid Derivatives may decrease the metabolism of Thiopurine Analogs. 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. Consider therapy modification

Adverse Reactions

>10%: Gastrointestinal: Diarrhea (11% to 17%)

1% to 10%:

Central nervous system: Depression (2%), dizziness (≤1%), vertigo (≤1%)

Dermatologic: Skin rash (2%), pruritus (1%)

Gastrointestinal: Abdominal cramps (≤10%), abdominal pain (≤10%), nausea (5%), bloating (2%), stomatitis (1%), vomiting (1%)

Neuromuscular & skeletal: Arthralgia (4%)

Respiratory: Upper respiratory tract infection (2%)

<1%, postmarketing, and/or case reports: Alopecia, anemia, angioedema, aplastic anemia, bloody stools, blurred vision, bronchospasm, cholestatic hepatitis, cholestatic jaundice, chest pain, chills, dehydration, dyspnea, dysuria, emotional lability, eosinophilia, epigastric distress, erythema, erythema nodosum, exacerbation of ulcerative colitis, fever, flatulence, hematuria, hemolytic anemia, hepatic cirrhosis, hepatitis, hepatic failure, hepatic necrosis, hot flash, hypermenorrhea, hypertension, impotence, increased gamma-glutamyl transferase, increased lactate dehydrogenase, increased serum alkaline phosphatase, increased serum ALT, increased serum AST, increased serum bilirubin, insomnia, interstitial nephritis, interstitial pneumonitis, irritability, jaundice, Kawasaki-like syndrome, leukopenia, local discomfort (rectal), lymphocytopenia, muscle cramps, myalgia, myocarditis, nephrotic syndrome, neutropenia, orthostatic hypotension, palpitations, pancreatitis, pancytopenia, paresthesia, pericarditis, peripheral edema, peripheral neuropathy, proteinuria, rectal hemorrhage, reticulocytosis, rigors, second degree atrioventricular block, skin photosensitivity, tachycardia, thrombocytopenia, tinnitus, tremor, urinary frequency, watery eyes, xerophthalmia, xerostomia

Warnings/Precautions

Concerns related to adverse effects:

  • Colitis: May exacerbate symptoms of colitis.
  • Diarrhea: A common adverse effect is diarrhea.

Disease-related concerns:

  • Asthma: Use with caution in patients with severe allergies or asthma.
  • Hepatic impairment: Use with caution in patients with hepatic impairment; monitor closely.
  • Renal impairment: Use with caution in patients with renal impairment; monitor closely.

Special populations:

  • Elderly: Use with caution.

Monitoring Parameters

CBC; hepatic function at baseline; renal function at baseline, 6 and 12 months during treatment, and annually thereafter (Cunliffe 2001); stool frequency; improvement in signs/symptoms of ulcerative colitis

Pregnancy

Pregnancy Risk Factor

C

Pregnancy Considerations

Animal studies have demonstrated fetal developmental toxicities. There are no well-controlled studies in pregnant women. Use during pregnancy only if clearly necessary.

Patient Education

  • Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
  • Patient may experience abdominal pain, abdominal cramps, nausea, or headache. Have patient report immediately to prescriber signs of kidney problems (unable to pass urine, blood in the urine, change in amount of urine passed, or weight gain) or diarrhea (HCAHPS).
  • Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

Source: Wolters Kluwer Health. Last updated January 28, 2020.