pharmacopeia
GET
/api/v1/drug/mesalamine
2D structure
5-amino-2-hydroxybenzoic acid
SMILES C1=CC(=C(C=C1N)C(=O)O)O
InChIKey KBOPZPXVLCULAV-UHFFFAOYSA-N

Mechanism of action

Sourced from openFDA

The mechanism of action of mesalamine is not fully understood, but appears to be a topical anti-inflammatory effect on colonic epithelial cells. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways, that is, prostanoids, and through the lipoxygenase pathways, that is, leukotrienes and hydroxyeicosatetraenoic acids, is increased in patients with ulcerative colitis, and it is possible that mesalamine diminishes inflammation by blocking cyclooxygenase and inhibiting prostaglandin production in the colon.

CyclooxygenaseLipoxygenase

Indications

Sourced from openFDA
  • Mesalamine delayed-release tablets are indicated for the treatment of moderately active ulcerative colitis in adults. Limitations of Use : Safety and effectiveness of mesalamine delayed-release tablets beyond 6 weeks have not been established.ICD-10: K51.90

Contraindications

Sourced from openFDA
  • Mesalamine delayed-release tablets are contraindicated in patients with known or suspected hypersensitivity to salicylates or aminosalicylates or to any of the ingredients of mesalamine delayed-release tablets [see Warnings and Precautions (5.3) , Adverse Reactions (6.2) , and Description (11) ] .contraindicated

Dosage & administration

Sourced from openFDA

Important Administration Instructions : Do not substitute one mesalamine delayed-release tablets 800 mg tablet for two mesalamine delayed-release 400 mg oral products. (2.1) Evaluate renal function prior to initiation of mesalamine delayed-release tablets. (2.1, 5.1) Take on an empty stomach, at least 1 hour before and 2 hours after a meal. (2.1) Swallow whole; do not cut, break or chew the tablets. (2.1) Drink an adequate amount of fluids. (2.1, 5.7) Treatment of Moderately Active Ulcerative Colitis : Recommended dosage is 1,600 mg (two 800 mg tablets) three times daily for 6 weeks. (2.2) 2.1 Important Administration Instructions Do not substitute one mesalamine delayed-release 800 mg tablet for two mesalamine delayed-release 400 mg oral products [see Clinical Pharmacology (12.3) ] . Evaluate renal function prior to initiation of mesalamine delayed-release tablets. Take mesalamine delayed-release tablets on an empty stomach, at least 1 hour before and 2 hours after a meal [see Clinical Pharmacology (12.3) ] . Swallow mesalamine delayed-release tablets whole. Do not cut, break or chew the tablets. Drink an adequate amount of fluids [see Warnings and Precautions (5.7) ] . Intact, partially intact, and/or tablet shells have been reported in the stool; Instruct patients to contact their healthcare provider if this occurs repeatedly. Protect mesalamine delayed-release tablets from moisture.

Warnings & precautions

Sourced from openFDA

Renal Impairment : Assess renal function at the beginning to treatment and periodically during treatment. Evaluate the risks and benefits in patients with known renal impairment or taking nephrotoxic drugs; monitor renal function. Discontinue mesalamine delayed-release if renal function deteriorates. (5.1, 7.1, 8.6) Mesalamine-Induced Acute Intolerance Syndrome : Symptoms may be difficult to distinguish from an ulcerative colitis exacerbation; monitor for worsening symptoms; discontinue if acute intolerance syndrome suspected. (5.2) Hypersensitivity Reactions, including Myocarditis and Pericarditis : Evaluate patients immediately and discontinue if a hypersensitivity reaction is suspected. (5.3) Hepatic Failure : Evaluate the risks and benefits in patients with known liver impairment. (5.4) Severe Cutaneous Adverse Reactions : Discontinue at the first signs or symptoms of severe cutaneous adverse reactions or other signs of hypersensitivity and consider further evaluation. (5.5) Photosensitivity : Advise patients with pre-existing skin conditions to avoid sun exposure, wear protective clothing, and use a broad-spectrum sunscreen when outdoors. (5.6) Nephrolithiasis: Mesalamine-containing stones are undetectable by standard radiography or computed tomography (CT). Ensure adequate hydration during treatment. (5.7) Iron Content of Mesalamine Delayed-Release : Consider the iron content of mesalamine delayed-release in patients taking iron supplementation and those at risk of iron overload.

Adverse reactions

Sourced from openFDA

The following serious or clinically significant adverse reactions described elsewhere in labeling are: Renal Impairment [see Warnings and Precautions (5.1) ] Mesalamine-Induced Acute Intolerance Syndrome [see Warnings and Precautions (5.2) ] Hypersensitivity Reactions [see Warnings and Precautions (5.3) ] Hepatic Failure [see Warnings and Precautions (5.4) ] Severe Cutaneous Adverse Reactions [see Warnings and Precautions (5.5) ] Photosensitivity [see Warnings and Precautions (5.6) ] Nephrolithiasis [see Warnings and Precautions (5.7) ] The most common adverse reactions (≥2%) are headache, nausea, nasopharyngitis, abdominal pain, and worsening of ulcerative colitis. (6.1) To report SUSPECTED ADVERSE REACTIONS, contact Amneal Pharmaceuticals at 1-877-835-5472 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Mesalamine delayed-release 800 mg tablets have been evaluated in 896 patients with ulcerative colitis in controlled studies. Three six-week, active-controlled studies were conducted comparing mesalamine delayed-release 800 mg tablets 4.8 grams per day with mesalamine delayed-release tablets 400 mg 2.4 grams per day in patients with mildly to moderately active ulcerative colitis.

Use in specific populations

Sourced from openFDA

Geriatric Patients : Increased risk of blood dyscrasias; monitor complete blood cell counts and platelet counts. (8.5) 8.1 Pregnancy Risk Summary Limited published data on mesalamine use in pregnant women are insufficient to inform a drug-associated risk. No fetal harm was observed in animal reproduction studies of mesalamine in rats and rabbits at oral doses approximately 0.97 times (rat) and 1.95 times (rabbit) the recommended human dose (see Data ). The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data Reproduction studies with mesalamine were performed during organogenesis in rats and rabbits at oral doses up to 480 mg/kg/day. There was no evidence of harm to the fetus. These mesalamine doses were about 0.97 times (rat) and 1.95 times (rabbit) the recommended human dose of 4.8 grams per day, based on body surface area. 8.2 Lactation Risk Summary Mesalamine and its N-acetyl metabolite are present in human milk in undetectable to small amounts ( see Data ). There are limited reports of diarrhea in breastfed infants. There is no information on the effects of the drug on milk production.

Pharmacokinetics

Sourced from openFDA
Metabolism
Absorption Plasma concentrations of mesalamine (5-aminosalicylic acid; 5-ASA) and its metabolite, N-acetyl-5-aminosalicylic acid (N-Ac-5-ASA) are highly variable following administration of mesalamine delayed-release tablets. Following single dose oral administration of mesalamine delayed-release 800 mg tablet in healthy subjects (N = 139) under fasted conditions, the mean C max , AUC 8-48h and AUC 0-tldc values were 208 ng/mL, 2,296 ng.h/mL, and 2533 ng.h/mL, respectively.

Overdosage

Sourced from openFDA

Mesalamine delayed-release is an aminosalicylate, and symptoms of salicylate toxicity include nausea, vomiting and abdominal pain, tachypnea, hyperpnea, tinnitus, and neurologic symptoms (headache, dizziness, confusion, seizures). Severe salicylate intoxication may lead to electrolyte and blood pH imbalance and potentially to other organ (e.g., renal and liver) involvement. There is no specific antidote for mesalamine overdose; however, conventional therapy for salicylate toxicity may be beneficial in the event of acute overdosage and may include gastrointestinal tract decontamination to prevent of further absorption. Correct fluid and electrolyte imbalance by the administration of appropriate intravenous therapy and maintain adequate renal function. Mesalamine delayed-release tablets are a pH dependent product and this factor should be considered when treating a suspected overdose.

Approval history

Sourced from openFDA
  • Dec 24, 1987NDANDA019618Mylan Speciality Lp
  • May 10, 1993NDANDA020049Takeda Pharms Usa
  • Jan 5, 2001NDANDA021252Abbvie
  • Sep 17, 2004ANDAANDA076751Padagis Israel
  • Jan 16, 2007NDANDA022000Takeda Pharms Usa
  • Oct 31, 2008NDANDA022301Salix
  • Jun 5, 2017ANDAANDA091640Zydus Pharms
  • Jul 21, 2017ANDAANDA203286Zydus Pharms

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
54,795 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Off Label Use9,02216%
  2. 2Drug Ineffective7,01613%
  3. 3Colitis Ulcerative6,52512%
  4. 4Diarrhoea4,8418.8%
  5. 5Condition Aggravated4,5278.3%
  6. 6Fatigue3,7726.9%
  7. 7Abdominal Pain3,6776.7%
  8. 8Haematochezia3,5826.5%
  9. 9Nausea3,2656.0%
  10. 10Headache3,0805.6%
  11. 11Arthralgia2,8975.3%
  12. 12Pyrexia2,8565.2%
  13. 13Crohn^s Disease2,7795.1%
  14. 14Weight Decreased2,6894.9%
  15. 15Pain2,6454.8%

Literature

View JSON

Recent PubMed references pinned to Mesalamine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 223 ClinicalTrials.gov registrations naming Mesalamine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Pharmacogenomics

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CPIC-curated drug–gene pairs for Mesalamine. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

Frequently asked questions

How does Mesalamine work?
The mechanism of action of mesalamine is not fully understood, but appears to be a topical anti-inflammatory effect on colonic epithelial cells. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways, that is, prostanoids, and through the lipoxygenase pathways, that is, leukotrienes and hydroxyeicosatetraenoic acids, is increased in patients with ulcerative colitis, and it is possible that mesalamine diminishes inflammation by blocking cyclooxygenase and inhibiting prostaglandin production in the colon.
What is Mesalamine used for?
According to FDA labeling, Mesalamine carries indications including: Mesalamine delayed-release tablets are indicated for the treatment of moderately active ulcerative colitis in adults. Limitations of Use : Safety and effectiveness of mesalamine delayed-release tablets beyond 6 weeks have not been established.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Mesalamine?
Mesalamine is classified as Aminosalicylic acid and similar agents, Aminosalicylate, Cyclooxygenase Inhibitors, Lipoxygenase Inhibitors, Decreased Leukotriene Activity, Decreased Platelet Aggregation, Decreased Prostaglandin Production, Decreased Thromboxane Production.
What are the brand names for Mesalamine?
Mesalamine is marketed under brand names including Apriso, Canasa, Delzicol, Lialda, Pentasa, Rowasa.
What are the contraindications for Mesalamine?
Mesalamine labeling lists contraindications including: Mesalamine delayed-release tablets are contraindicated in patients with known or suspected hypersensitivity to salicylates or aminosalicylates or to any of the ingredients of mesalamine delayed-release tablets [see Warnings and Precautions (5.3) , Adverse Reactions (6.2) , and Description (11) ] .. Always consult the full prescribing information and a clinician.
Note. Data for mesalamine is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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