Dosing & Uses
Dosage Forms & Strengths
- 250mg (Pentasa)
- 375mg (Apriso)
- 500mg (Pentasa)
- 400mg (Asacol)
- 800mg (Asacol HD)
- 1.2g (Lialda)
- 400mg (Delzicol)
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
- 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
- 400mg (Asacol)
- 400mg (Delzicol)
Asacol or Delzicol: Indicated for mildly to moderately active ulcerative colitis in children aged ≥5 yr
- Safety and efficacy not established
- 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
Serious - Use Alternative
Significant - Monitor Closely
Abdominal pain (4-8%)
GI discomfort (4-8%)
Exacerbation of colitis (3%)
Frequency Not Defined
Creatinine clearance decreased
Mesalamine-induced acute intolerance syndrome
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, renal failure, minimal change nephropathy
Respiratory, thoracic and mediastinal disorders: Hypersensitivity pneumonitis (including interstitial pneumonitis, allergic alveolitis, eosinophilic pneumonitis)
Skin: Psoriasis, pyoderma gangrenosum, erythema nodosum
Urogenital: Reversible oligospermia
Hypersensitivity to mesalamine or salicylates
Rectal suspension: Hypersensitivity to salicylates, aminosalicylates or to any ingredients in the suppository vehicle
Children with chickenpox or flulike symptoms
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; evaluate renal function prior to initiation of therapy and periodically while on therapy
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
Pregnancy & Lactation
Pregnancy: Limited published data on mesalamine use in pregnant women are insufficient to inform a drug-associated risk; no evidence of teratogenicity was observed in rats or rabbits when treated during gestation with orally administered mesalamine at doses greater than the recommended human intra-rectal dose
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; mesalamine and its N-acetyl metabolite are present in human milk in undetectable to small amounts; there are limited reports of diarrhea in breastfed infants; there is no information on effects of drug on milk production; monitor breastfed infants for diarrhea
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.
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
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)
Protein bound: 43% (5-ASA); 78% (N-acetyl-5-ASA)
Vd: 0.2 L/kg
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)
Half-life: 0.5-10 hr (5-ASA); 2-15 hr (N-acetyl-5-ASA )
Excretion: Feces 72%; urine: 19-30%
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
- 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
- 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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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.
|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.|
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
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Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.