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Mesalamine

    DEA Class; Rx

    Common Brand Names; Pentasa, Delzicol, Lialda, Apriso, Asacol HD (DSC)

    • 5-Aminosalicylic Acid Derivatives

    mesalamine rectal (Rx)

    Brand and Other Names: Canasa, Rowasa
    • Classes: 5-Aminosalicylic Acid Derivatives

    5-aminosalicylate (5-ASA); available in oral and rectal formulations; clinical response is due to local effect
    Used as an anti-inflammatory agent for ulcerative colitis; not considered effective for Crohn’s disease
    Also used for ulcerative proctitis (rectal formulations, suppository and enema only)

    Indicated for the treatment of mildly to moderately active ulcerative colitis.

    For the treatment of active ulcerative proctitis.
     

    Hypersensitivity to mesalamine or salicylates

    Breastfeeding

    Rectal suspension: Hypersensitivity to salicylates, aminosalicylates or to any ingredients in the suppository vehicle

    Children with chickenpox or flulike symptoms

    • 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%)

    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

    Renal impairment, including minimal change nephropathy, acute and chronic interstitial nephritis, and renal failure, reported; cases of nephrolithiasis reported; mesalamine-containing stones are radiotransparent and undetectable by standard radiography or computed tomography (CT); ensure adequate fluid intake during treatment; evaluate renal function prior to initiation of therapy and periodically while on therapy

    Evaluate renal function in all patients prior to initiation and periodically while on therapy; the risk of adverse reactions to this drug may be greater in patients with impaired renal function; mesalamine is known to be substantially excreted by the kidney; evaluate the risks and benefits in patients with known renal impairment or taking nephrotoxic drugs; monitor renal function

    Acute intolerance syndrome may occur; symptoms include cramping, abdominal pain, bloody diarrhea, and sometimes fever, headache, malaise, pruritis, rash, conjunctivitis, and 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

    Pregnancy: Limited published data on mesalamine use in pregnant women are insufficient to inform a drug-associated risk

    Lactation: Developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on the breastfed child from therapy or from underlying maternal conditions

    Adults

    4 grams/day PR for rectal enema; 1 gram/day PR for rectal suppositories. For oral products: 1.5 grams/day PO for extended-release capsules (i.e., Apriso); 2.4 grams/day PO for delayed-release tablets or capsules (i.e, Delzicol); 4 grams/day PO for controlled-release capsules (i.e., Pentasa); 4.8 grams/day PO for delayed-release tablets (i.e., Asacol HD, Lialda).

    Geriatric

    4 grams/day PR for rectal enema; 1 gram/day PR for rectal suppositories. For oral products: 1.5 grams/day PO for extended-release capsules (i.e., Apriso); 2.4 grams/day PO for delayed-release tablets or capsules (i.e, Delzicol); 4 grams/day PO for controlled-release capsules (i.e., Pentasa); 4.8 grams/day PO for delayed-release tablets (i.e., Asacol HD, Lialda).

    Adolescents

    Delzicol – Maximum dosage determined by weight:
    54 to 90 kg: 44 mg/kg/day PO (Max: 2.4 grams/day)
    33 to 53 kg: 61 mg/kg/day PO (Max: 2 grams/day)
    17 to 32 kg: 71 mg/kg/day PO (Max: 1.2 grams/day)
     
    Lialda – Maximum dosage determined by weight:
    More than 50 kg: 4.8 grams/day PO
    More than 35 kg to 50 kg: 3.6 grams/day PO
    24 kg to 35 kg: 2.4 grams/day PO

    Children

    5 to 12 years: Maximum dosage determined by weight and product chosen:
    Delzicol
    54 to 90 kg: 44 mg/kg/day PO (Max: 2.4 grams/day)
    33 to 53 kg: 61 mg/kg/day PO (Max: 2 grams/day)
    17 to 32 kg: 71 mg/kg/day PO (Max: 1.2 grams/day)
     
    Lialda
    More than 50 kg: 4.8 grams/day PO
    More than 35 kg to 50 kg: 3.6 grams/day PO
    24 kg to 35 kg: 2.4 grams/day PO
     
     
    1 to 4 years: Safety and efficacy have not been established; off-label use reported for some formulations in children as young as 4 years of age.

    Infants

    Safety and efficacy have not been established.

    Mesalamine 

    capsule, extended-release

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

    tablet, delayed-release

    • 1.2g (Lialda, generic)

    capsule, delayed-release

    • 400mg (Delzicol, generic)

    rectal suppository

    • 1g (Canasa)

    rectal suspension enema

    • 4g/60mL (Rowasa)