Names and pronunciation
(me-sal′a-meen) Apriso, Asacol , Ascol DR , Asacol HD, Canasa, Delzicol, Lialda, Mezavant , Pentasa, Rowasa, Salofalk , SfRowasa
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Drug reference
(me-sal′a-meen) Apriso, Asacol , Ascol DR , Asacol HD, Canasa, Delzicol, Lialda, Mezavant , Pentasa, Rowasa, Salofalk , SfRowasa
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Func. class.: GI antiinflammatory
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Chem. class.: 5-Aminosalicylic acid
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Do not confuse: Asacol/Os-Cal
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ACTION: May diminish inflammation by blocking cyclooxygenase, inhibiting prostaglandin production in colon; local action only
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USES: Mild to moderate active distal ulcerative colitis, proctitis, proctosigmoiditis
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CONTRAINDICATIONS: Hyper- sensitivity to this product or salicylates, 5-aminosalicylates Precautions: Pregnancy, breastfeeding, children, geriatric patients, renal dis- ease, sulfite sensitivity, pyloric stenosis, GI obstruction
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SIDE EFFECTS CNS: dizziness, Headache, fever, insomnia, asthenia, weakness, fatigue CV: Chest pain, palpitations, pericarditis EENT: Pharyngitis, rhinitis GI: Cramps, gas, nausea, diarrhea, rectal pain, constipation, vomiting, pancreatitis GU: Nephrotoxicity, interstitial nephritis INTEG: Rash, itching, acne, Stevens- Johnson syndrome, hair loss SYST: Anaphylaxis, acute intolerance syndrome, angioedema, DRESS
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INTERACTIONS Increase: action, adverse reactions of azaTHIOprine, mercaptopurine Decrease: mesalamine absorption— lactulose, antacids Decrease: effect of—warfarin Drug/Lab Test Increase: AST, ALT, alk phos, LDH, GGTP, amylase, lipase, BUN, serum creatinine
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DOSAGE AND ROUTES Treatment of ulcerative colitis • Adult: RECT 60 mL (4 g) at bedtime, retained for 8 hr × 3-6 wk; DEL REL TAB (Lialda) 2.4-4.8 g/day × 8 wk; DEL REL TAB (Asacol HD) 1.6 g × 6 wk; DEL REL TAB (Asacol) 800 mg tid × 6 wk; CONTROLLED REL CAP (Pen- tasa) 1 g qid up to 8 wk; RECT SUPP 500 mg bid retained for 1-3 hr × 3-6 wk until remission, may increase tid if needed; DEL REL CAP (Delzicol) 800 mg tid × 6 wk • Child ⬧5 yr and 54-90 kg: PO Delzicol 27-44 mg/kg/day in divided doses × 6 wk, max 2.4 g/day • Child ⬧5 yr and 33-53 kg: PO Delzicol 37-61 mg/kg/day in 2 divided doses × 6 wk, max 2 g/day • Child ⬧5 yr and 17-32 kg PO: Delzicol 36-71 mg/kg/day in 2 divided doses × 6 wk, max 1.2 g/day Maintenance of remission • Adult: DEL REL TAB (Asacol) 800 mg bid or 400 mg qid; DEL REL TAB (Apriso) 1500 mg (4 caps) each AM; DEL REL TAB (Lialda) 2.4 g (2 tabs) daily with meal; DEL REL TAB (Delzi- col) 800 mg bid; Pentasa Adult 1000-mg capsules qid (4 g) × 8 wk Treatment of ulcerative proctosis- moiditis/proctitis • Adult: Rectal Rowasa 4 g enema (60 mL) at bedtime retained for 8 hr × 3-6 wk
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Available forms: Rectal susp 4 g/60 mL (Rowasa); ext rel tab 500 mg; ext rel cap 250, 500 mg (Pentasa); 0.375 g (Apriso); del rel tab 400 mg (Asacol), 800 mg (Asacol HD); del rel tab (Lialda) 1.2 g; rectal supp 1000 mg (Canasa); del rel cap (Delzicol) 400 mg; enema sus- pension 4 g/60 mL (SfRowasa)
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Administer: PO route • Swallow tabs whole; do not break, crush, or chew tabs; give with a full glass of water • Lialda: take with meal • Apriso caps: take without regard to meals in AM • Delzicol caps: give ≥1 hr before a meal or 2 hr after a meal Rectal suspension • Product should be given at bedtime, retained until morning (8 hr); empty bowel before insertion, shake well Rectal suppository • Moisten before insertion; suppository should be retained for 1-3 hr
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Assess: • Allergy to salicylates, sulfonamides, sulfites: if allergic reactions occur, dis- continue product • Renal studies: BUN, creatinine before, periodically during treatment; renal tox- icity may occur; increase fluids to main- tain urine at ≥1200 mL/day to prevent crystalluria • Bowel disorders: cramps, gas, nausea, diarrhea, rectal pain; if severe, product should be discontinued • Pregnancy/breastfeeding: avoid in pregnancy; excreted in breast milk, avoid use
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Evaluate: • Therapeutic response: absence of pain, bleeding from GI tract, decrease in number of diarrhea stools
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To report immediately trouble breath- ing, rash, hives • To use rectal dose at bedtime, teach how to use • That follow-up exams and blood work will be needed, including possible proc- toscopy or sigmoidoscopy • Not to drive or engage in other hazard- ous activities until response is known, dizziness may occur • That usual initial course of therapy is 3-6 wk; to notify prescriber if symptoms do not improve after 2 mo of treatment; to continue to take even if feeling better; not to miss doses; if a dose is missed, to take when remembered, if almost time for next dose, skip it; do not double doses • To shake bottle well (rectal susp) • About method of rectal administration • To inform prescriber of GI symptoms • To report abdominal cramping, pain, diarrhea with blood, headache, fever, rash, chest pain, bruising, bleeding, mouth sores; product should be discontinued
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PHARMACOKINETICS RECT: Primarily excreted in feces unchanged but some in urine as metabo- lite; half-life 1 hr, metabolite half-life 12 hr PO, 1⁄2-11⁄2 hr rectal
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• Child ⬧5 yr and 54-90 kg: PO Delzicol 27-44 mg/kg/day in divided doses × 6 wk, max 2.4 g/day
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• Child ⬧5 yr and 33-53 kg: PO Delzicol 37-61 mg/kg/day in 2 divided doses × 6 wk, max 2 g/day
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• Child ⬧5 yr and 17-32 kg PO: Delzicol 36-71 mg/kg/day in 2 divided doses × 6 wk, max 1.2 g/day Maintenance of remission
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