mesalamine (Rx)

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Brand and Other Names:Asacol HD, Pentasa, more...Delzicol, Lialda, Apriso

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule, extended-release

  • 250mg (Pentasa)
  • 375mg (Apriso)
  • 500mg (Pentasa)

tablet, delayed-release

  • 400mg (Asacol)
  • 800mg (Asacol HD)
  • 1.2g (Lialda)

capsule, delayed-release

  • 400mg (Delzicol)
more...

Ulcerative Colitis

Remission induction of active, mild to moderate disease

  • Asacol HD: 1.6 g PO three times daily
  • Delzicol: 800 mg PO three times daily 1 hr ac or 2 hr pc
  • Lialda: 2.4-4.8 g PO qDay with meal up to 8 weeks
  • Pentasa: 1 g PO four times daily for 8 weeks

Remission maintenance

  • Apriso: 1.5 g PO qDay in am
  • Delzicol: 1.6 g/day PO in divided doses 1 hr ac or 2 hr pc
  • Asacol: 1.6 g/day PO in divided doses 1 hr ac or 2 hr pc
  • Lialda: 2.4 g PO qDay with food
  • Pentasa: 1 g/day PO four times daily for up to 8 weeks

Crohn Disease (Off-label)

Remission induction of active, mild-to-moderate disease

Asacol HD: 1.6 g three times daily

Lialda: 2.4-4.8 g PO qDay with meal for up to 8 weeks

Pentasa: 1 g PO four times daily for 8 weeks

Dosage Forms & Strengths

tablet, delayed-release

  • 400mg (Asacol)

capsule, delayed-release

  • 400mg (Delzicol)
more...

Ulcerative Colitis

Asacol or Delzicol: Indicated for mildly to moderately active ulcerative colitis in children aged ≥5 yr

<5 years

  • Safety and efficacy not established

≥5 years

  • Duration of treatment: 6 weeks
  • 17 to <33 kg: 36-71 mg/kg/day PO divided twice daily; not to exceed 1.2 g/day
  • 33 to <54 kg: 37-61 mg/kg/day PO divided twice daily; not to exceed 2 g/day
  • 54 to 90 kg: 27-44 mg/kg/day PO divided twice daily; not to exceed 2.4 g/day
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Interactions

Interaction Checker

and mesalamine

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            1-10%

            Abdominal pain (4-8%)

            GI discomfort (4-8%)

            Headache (7%)

            Flatulence (1-6%)

            Nausea (1-6%)

            Fatigue (3%)

            Asthenia (3%)

            Malaise (3%)

            Weakness (3%)

            Fever (3%)

            Exacerbation of colitis (3%)

            Dizziness (2-3%)

            Rash (1-3%)

            Pruritus (1-3%)

            Acne (1-3%)

            Frequency Not Defined

            Pericarditis (rare)

            Pharyngitis

            Sensitivity reaction

            Cholestatic hepatitis

            Creatinine clearance decreased

            Flulike syndrome

            Discolored urine

            Postmarketing Reports

            Body as a whole: Lupus-like syndrome, drug fever

            Cardiac disorders: Pericarditis, pericardial effusion, myocarditis

            Gastrointestinal: Pancreatitis, cholecystitis, gastritis, gastroenteritis, gastrointestinal bleeding, perforated peptic ulcer

            Hepatic: Jaundice, cholestatic jaundice, hepatitis, liver necrosis, liver failure, Kawasaki-like syndrome including changes in liver enzymes

            Hematologic: Agranulocytosis, aplastic anemia

            Immune system disorders: Anaphylactic reaction, Stevens-Johnson syndrome (SJS), drug reaction with eosinophilia and systemic symptoms (DRESS), angioedema

            Musculoskeletal and connective tissue disorders: Myalgia

            Neurological/psychiatric: Peripheral neuropathy, Guillain-Barre syndrome, transverse myelitis

            Renal disorders: Interstitial nephritis

            Respiratory, thoracic and mediastinal disorders: Hypersensitivity pneumonitis (including interstitial pneumonitis, allergic alveolitis, eosinophilic pneumonitis)

            Skin: Psoriasis, pyoderma gangrenosum, erythema nodosum

            Urogenital: Reversible oligospermia

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            Warnings

            Contraindications

            Hypersensitivity to mesalamine or salicylates

            Breastfeeding

            Rectal suspension: Patients with history of sulfite hypersensitivity

            Children with chickenpox or flulike symptoms

            Cautions

            Sulfasalazine hypersensitivity, renal insufficiency, coagulation abnormalities, pyloric stenosis

            Use caution in active PUD, severe renal failure

            Do not use with lactulose or drugs that lower intestinal pH

            Although pericarditis rarely occurs, investigate any chest pain or dyspnea

            Oligospermia has been reported in males

            Hepatic failure may occur, particularly with preexisting liver impairment

            May lead to falsely elevated test results when measuring urinary normetanephrine by liquid chromatography with electrochemical detection, because of the similarity in the chromatograms of normetanephrine and mesalamine’s main metabolite, N-acetyl aminosalicylic acid; an alternative, selective assay for normetanephrine should be considered

            Worsening of colitis/IBD may occur following initiation of therapy

            Evaluate renal function prior to initiation of Asacol HD

            Evaluate the risks and benefits in patients with known renal impairment or taking nephrotoxic drugs; monitor renal function

            Acute intolerance syndrome may occur; symptoms may be difficult to distinguish from an ulcerative colitis exacerbation; monitor for worsening symptoms; discontinue if acute intolerance syndrome suspected

            Hypersensitivity reactions, including myocarditis and pericarditis reported; evaluate patients immediately and discontinue if hypersensitivity reaction suspected

            Evaluate the risks and benefits in patients with known liver impairment

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            Pregnancy & Lactation

            Pregnancy category: B/C dependent on dosage form

            Lactation: Not known whether drug or metabolites are distributed into breast milk; use caution

            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.

            more...
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            Pharmacology

            Mechanism of Action

            Anti-inflammatory agent; mesalamine (5-aminosalicylic acid) is the active component of sulfasalazine, but specific MOA is unknown; probably inhibits prostaglandin and leukotriene synthesis and release in colon

            Absorption

            Bioavailability: Immediate-release is extensively and rapidly absorbed; extended-release 20-30% absorbed

            Onset: Improvement usually evident in 1 week-3 months

            Peak serum time: 4 hr (Apriso); 3 hr (Pentasa); 4-16 hr (Delzicol); 4-7 hr (rectal); 9-12 hr (Lialda); 8 hr (Mezavant); 4-12 hr (Asacol); 10-16 hr (Asacol HD)

            Distribution

            Protein bound: 43% (5-ASA); 78% (N-acetyl-5-ASA)

            Vd: 0.2 L/kg

            Metabolism

            Rapidly acetylated in colon wall and liver, independent of pt acetylator status, into N-acetyl-5-aminosalicylic acid

            Metabolites: N-acetyl-5-aminosalicylic acid (inactive)

            Elimination

            Half-life: 0.5-10 hr (5-ASA); 2-15 hr (N-acetyl-5-ASA )

            Excretion: Feces 72%; urine: 19-30%

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            Administration

            Instructions

            Apriso, Asacol HD: May take with or without food

            Delzicol: Take 1 hr before or 2 hr after meals

            Lialda: Take with food

            Do not substitute one Asacol HD 800 tablet for two mesalamine delayed-release 400 mg oral products

            Swallow whole; do not chew, break, or crush

            Patients unable to swallow tablet or capsule whole

            • Pentasa
              • Capsules may, alternatively, be opened and the entire contents sprinkled onto applesauce or yogurt
              • The entire contents should be consumed immediately; the capsules and capsule contents must not be crushed or chewed
            • Delzicol
              • For patients who are unable to swallow the capsules whole, carefully open the capsule(s) and swallow the contents (four 100 mg tablets)
              • Open the number of capsules required to make up a complete dose
              • There are 4 tablets per capsule; ensure all tablets per capsule are swallowed and no tablets are retained in the mouth
              • Swallow the tablets whole; do not cut, break, crush or chew the tablets
              • Intact, partially intact, and/or tablet shells have been reported in the stool; instruct patients to contact their physician if this occurs repeatedly
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            Formulary

            FormularyPatient Discounts

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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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