olsalazine (Rx)

Brand and Other Names:Dipentum
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 250mg

Ulcerative Colitis

Maintenance: 1g PO qDay in 2 divided doses

Administration

Take with food

Other Indications & Uses

Maintenance of remission of ulcerative colitis in patients who are intolerant of sulfasalazine

Safety & efficacy not established

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Adverse Effects

>10%

Diarrhea (17%)

Abdominal pain (11%)

1-10%

Nausea/vomiting (6%)

Headache (5%)

Arthralgia (4%)

Dyspepsia (4%)

Joint pain (4%)

Rash/itching (3.6%)

Fatigue (1.8%)

Bloating (1.5%)

Depression (1.5%)

Upper respiratory infection (1.5%)

Anorexia (1.3%)

Dizziness (1%)

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Warnings

Contraindications

Patients with known or suspected hypersensitivity to salicylates, aminosalicylates or their metabolites, or excipients

Cautions

Mesalamine-induced acute intolerance syndrome may occur; drug is converted to mesalamine, which has been associated with acute intolerance syndrome that may be difficult to distinguish from exacerbation of ulcerative colitis; symptoms include cramping, acute abdominal pain and bloody diarrhea, sometimes fever, headache, and rash; monitor patients for worsening of symptoms while on treatment; discontinue therapy if acute intolerance syndrome suspected

Some patients who have experienced a hypersensitivity reaction to sulfasalazine have similar reaction to drug or to other compounds that contain or are converted to mesalamine; mesalamine-induced hypersensitivity reactions may present as internal organ involvement, including myocarditis, pericarditis, nephritis, hepatitis, pneumonitis, and hematologic abnormalities; evaluate patients immediately if signs or symptoms of a hypersensitivity reaction present; discontinue therapy if an alternative etiology for signs and symptoms cannot be established

There have been reports of hepatic failure in patients with pre-existing liver disease receiving therapy; because drug is converted to mesalamine, evaluate risks and benefits of therapy in patients with known liver impairment

Patients with pre-existing skin conditions such as atopic dermatitis and atopic eczema have reported more severe photosensitivity reactions when receiving therapy; advise patients to avoid sun exposure, wear protective clothing, and use a broad-spectrum sunscreen when outdoors

Cases of nephrolithiasis have been reported with use of mesalamine; active moiety in drug, including stones with 100% mesalamine content; mesalamine-containing stones are radiotransparent and undetectable by standard radiography or computed tomography (CT); ensure adequate hydration during treatment

Renal toxicity

  • Renal impairment, including minimal change disease, acute and chronic interstitial nephritis, and renal failure reported in patients given products that contain mesalamine or are converted to mesalamine; in animal studies, kidney was principal organ of mesalamine toxicity
  • Evaluate the risks and benefits of therapy in patients with known renal impairment or a history of renal disease or taking concomitant nephrotoxic drugs
  • Mesalamine is known to be substantially excreted by kidney, and risk of adverse reactions may be greater in patients with impaired renal function
  • Evaluate renal function in all patients prior to initiation and periodically while on therapy
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Pregnancy & Lactation

Pregnancy Category: C

Lactation

Not known whether drug distributed into breast milk, use caution

5-ASA is excreted in breast milk & may cause diarrhea in infant

However little is absorbed from oral olsalazine

Avoid

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

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Pharmacology

Mechanism of Action

Converted to 5-aminosalicylic acid (mesalamine) by gastrointestinal flora which is thought to be the therapeutically active component; works topically rather tha systemically

Absorption

~2.4% of a single 1 g dose

Peak plasma (single 1 g dose)

  • Olsalazine: 1.6-6.2 umol/L
  • 5-aminosalicylic acid (5-ASA): 0-4.3umol/L
  • N-acetyl-5-ASA: 1.7-8.7 umol/L

Distribution

Protein bound: 99%

Metabolism

>90% converted to 5-ASA in the gut

5-ASA is deactivated to N-Ac-5-ASA in colonic epithelium & liver

Approx. 0.1% converted to olsalazine-O-sulfate (Olsalazine-S) in liver

Elimination

Half-Life

  • Olsalazine: 0.9 hr
  • 5-ASA: 45 min
  • N-Ac-5-ASA: 80 min
  • Olsalazine-S (~0.1%): 7 d

Excretion

  • Urine: 20% (mostly N-Ac-5-ASA)
  • Feces: 80% (both 5-ASA & N-Ac-5-ASA)
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Formulary

FormularyPatient Discounts

Adding plans allows you to compare formulary status to other drugs in the same class.

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The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

Tier Description
1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
NC NOT COVERED – Drugs that are not covered by the plan.
Code Definition
PA Prior Authorization
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
QL Quantity Limits
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
ST Step Therapy
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
OR Other Restrictions
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.