What is Pentasa (Mesalamine)?
Pentasa (mesalamine) for oral administration is an extended-release formulation of mesalamine. Mesalamine is an aminosalicylate anti-inflammatory agent used for the induction of remission and treatment of mild to moderate ulcerative colitis in adults.
How does Pentasa work?
The detailed mechanisms of Pentasa are not well understood, but it does show a topical anti-inflammatory effect on epithelial cells in the colon. Arachidonic acid metabolites (e.g., prostaglandins, leukotrienes) are increased in ulcerative colitis patients, and it is postulated that Pentasa reduces inflammation by inhibiting cycloxygenase and reducing prostaglandin production in the colon.
Dosage and How to Use
Pentasa extended-release capsules are available in the following dosages:
- 250 mg capsules
- 500 mg capsules
For the induction of remission and treatment of mild to moderate ulcerative colitis in adults, the recommended dosage is 1g (4 x 250 mg capsules or 2 x 500 mg capsules) four times daily (4 grams total daily dosage).
Pentasa capsules can be swallowed whole, or the capsule can be opened to sprinkle the entire contents onto applesauce or yogurt and consumed immediately. The capsule or capsule contents must never be crushed or chewed.
Patients should drink plenty of fluids while treated with Pentasa.
Store at room temperature (25°C or 77°F). Temperature excursions are permitted between 15°C to 30°C (59°F to 86°F). Keep out of sight and reach of children.
If overdosage with Pentasa occurs, seek medical attention immediately.
In the case of overdosage, signs of salicylate toxicity are possible (nausea, vomiting, abdominal pain, tachypnea, tinnitus, headache, dizziness, or confusion). Severe salicylate toxicity has the potential to cause electrolyte and blood pH imbalances and may lead to organ damage.
There is no specific antidote for Pentasa overdose, but conventional salicylate toxicity treatment may be beneficial. Potential interventions may include gastrointestinal tract decontamination to reduce absorption, followed by correction of fluids and electrolytes.
The possible side effects of Pentasa are:
- Abdominal pain, vomiting, nausea, diarrhea
- Back pain
- Muscle and joint pain
Rare but serious side effects of Pentasa are:
Serious skin reactions
Stevens-Johnson syndrome (SJS) and toxic epidermal necrosis (TEN) have been reported in patients taking Pentasa. Seek immediate medical attention and stop taking Pentasa if you have one of the following signs of a severe skin reaction: mouth sores, severe skin rash, or any other sign of an allergic reaction.
Kidney problems and kidney stones
Patients taking Pentasa can develop kidney stones and other kidney issues. Contact your doctor if you have any of the following signs of kidney problems: blood in the urine, more frequent urination, or pain in your back, side, or groin. Make sure to drink plenty of fluids while taking Pentasa. Your doctor will be able to give you more information on how much water you should be drinking.
Acute intolerance syndrome
Symptoms can be similar to a flare of inflammatory bowel disease. Contact your doctor immediately if you are experiencing a flare-up of your condition.
This can include myocarditis, pericarditis, shortness of breath, or swelling in the legs and feet
Liver problems, including liver failure
Contact your doctor immediately if you see any of the following signs of liver failure: yellowing of the skin and eyes, dark urine, pale stool, nausea, loss of appetite, or pain in the upper right area of the stomach.
This is not a comprehensive list of side effects. Please ask your doctor or pharmacist for more information. Contact your doctor immediately if you believe you are experiencing a serious side effect.
Warnings & Precautions
Use Pentasa with caution in patients with pre-existing skin conditions like dermatitis or eczema due to the risk of more severe photosensitivity reactions. Patients should avoid prolonged sun exposure and use protective clothing and sunscreen when outdoors.
Hepatic failure has been reported in patients with pre-existing liver conditions. Carefully evaluate the risks versus the benefits of treatment with Pentasa in patients with known liver impairment.
Kidney stones and other kidney problems have been reported in patients taking Pentasa. Use caution in patients with renal impairment and ensure adequate hydration during treatment.
Drug Interactions & Other Interactions
Nephrotoxic agents, including non-steroidal anti-inflammatory drugs (NSAIDs)
Using mesalamine with nephrotoxic agents (e.g., NSAIDs) may increase the risk of nephrotoxicity. Monitor patients for changes in renal function if taking NSAIDs and mesalamine concurrently.
Azathioprine or 6-mercaptopurine
Using mesalamine with any drugs known to cause myelotoxicity (e.g., azathioprine and 6-mercaptopurine) may increase the risk for blood disorders, bone marrow failure, and associated complications. Carefully monitor blood tests if concurrent mesalamine and azathioprine or 6-mercaptopurine use is necessary.
Pentasa is contraindicated in patients with hypersensitivity to mesalamine, aminosalicylates, salicylates, or any component of the formulation.