Mesalamine
PENTASA
Pronunciation: me-SAL-a-meen
“My salami (has) A.S.A. for ass and colon”
Mesalamine (5-ASA) and aspirin (ASA) are both derivatives of salicylic acid
Pentasa release is time-dependent: hits small intestine and beyond
Asacol release is pH-dependent, delivering 5-ASA to colon
What it isTopical colonic 5-aminosalicylate with PPAR-gamma agonism and 5-lipoxygenase inhibition; ulcerative colitis.
Why it mattersIt works locally, and each delivery system determines which bowel segment receives the drug.
What it changesInterstitial nephritis requires periodic creatinine monitoring. Formulations are not interchangeable because release sites differ.
FDA-approved for
- ulcerative colitis
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Mildly to moderately active ulcerative colitis (induction of remission and treatment) | Adult | 1 g QID (4 × 250 mg or 2 × 500 mg caps) | 1 g QID | 1 g QID (4 g/day) |
Renal Evaluate renal function before and periodically; weigh risk/benefit and monitor in known impairment; discontinue if renal function deteriorates (no dose adjustment given)
Hepatic Caution — hepatic failure reported with mesalamine in pre-existing liver disease; weigh risk/benefit (no dose adjustment given)
Instructions
- Swallow capsules whole; do not crush or chew
- Alternatively open and sprinkle entire contents on applesauce or yogurt; consume immediately
- Drink adequate fluids
Available strengths
- ER cap 250, 375, 500 mg
- cap 250, 500 mg
- DR cap 400 mg
- DR tab 800, 1200 mg
- susp 4 g/60 mL
- enema 4 g/60 mL
- supp 1000 mg
Contraindications
- Known or suspected hypersensitivity to salicylates or aminosalicylates
Cautions
- Renal impairment (minimal change disease, interstitial nephritis, renal failure)
- Mesalamine-induced acute intolerance syndrome
- Hypersensitivity incl. myocarditis/pericarditis
- Hepatic failure in pre-existing liver disease
- Severe cutaneous adverse reactions (SJS/TEN, DRESS, AGEP)
- Photosensitivity
- Nephrolithiasis (radiolucent stones) — ensure hydration
- Interference with urinary normetanephrine assay
Adverse reactions
- Diarrhea (3%)
- Headache (2%)
- Nausea (2%)
- Abdominal pain (2%)
- Dyspepsia (2%)
- Vomiting (2%)
- Rash (1%)
Pregnancy Published data have not reliably shown association with major birth defects, miscarriage, or adverse outcomes; no fetal harm in rats/rabbits.
Lactation Mesalamine and N-acetyl metabolite present in milk in small amounts (RID ≤0.1%); diarrhea reported in breastfed infants — monitor.
Cost
| Strength | #/mo | generic $/mo | CostPlus | |
|---|---|---|---|---|
| 250 mg | ER cap | 30 qd | not offered | |
| 375 mg | ER cap | 30 qd | $14.34 | offered |
| 500 mg | ER cap | 30 qd | $104.11 | not offered |
Other forms: Mesalamine DR (LIALDA)
Generic entry2004
NO BOXED WARNINGS
Principal riskInterstitial nephritis
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.