Mesalamine

What is Mesalamine?

• Mesalamine (Apriso; Asacol; Asacol HD; Delzicol; Lialda; Pentasa) is an aminosalicylate used to treat ulcerative colitis (a condition which causes swelling and sores in the lining of the colon (large intestine) and rectum) and also to maintain improvement of ulcerative colitis symptoms

Mesalazine structure

What are the uses of this medicine?

Mesalamine (Apriso; Asacol; Asacol HD; Delzicol; Lialda; Pentasa) is used:

• for the treatment of mildly to moderately active ulcerative colitis in patients 5 years of age and older.
• for the maintenance of remission of ulcerative colitis in adults.

How does this medicine work?

• Mesalamine (me sal’ a meen) is used to treat disease flares in ulcerative colitis and to maintain disease remission.
• Mesalamine has antiinflammatory, antioxidant and antimicrobial activity and is locally active in the large intestine in reducing inflammation and injury.
• Mesalamine appears to act by inhibition of lipooxygenase activity, thereby inhibiting production of leukotrienes and leading to reduction in interleukin 1 (IL-1) and tumor necrosis factor (TNF) alpha.
• 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.

Who Should Not Use this medicine ?

This medicine have cannot be used in patients with:

• with known or suspected hypersensitivity to salicylates or aminosalicylates or to any of the ingredients.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention any of the following:

• antacids such as aluminum hydroxide and magnesium hydroxide (Maalox), calcium carbonate (Tums), or calcium carbonate and magnesium (Rolaids)
• aspirin or other nonsteroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen (Advil, Motrin) and naproxen (Aleve, Naprosyn)
• azathioprine (Azasan, Imuran)
• iron supplements
• mercaptopurine (Purinethol)

Is this medicine FDA approved?

• Mesalamine was approved for use in the United States in 1985 and remains a first line agent in the therapy of ulcerative colitis, both for induction and maintenance of clinical remission.
• It is poorly effective in Crohn disease, its major activity being in the large, rather than the small intestine.
• Mesalamine by itself is largely absorbed in the small intestine and little reaches the colon.
• For this reason, it is formulated to avoid absorption in the upper intestine and to be released in active form in the colon.
• The delayed absorption is accomplished either by enteric coating or by formulation as a pro-drug that is activated in the large intestine by local conditions or bacterial enzymes.
• Formulations of mesalamine include extended or delayed release formulations (Pentasa, Asacol, Lialda, Apriso) and mesalamine pro-drugs including sulfasalazine, olsalazine and balsalazide.

How should this medicine be used?

Recommended dosage:

• Typical doses range considerable and vary by preparation, but are generally in the range of 1.5 to 4.8 g of mesalamine daily.

Treatment of Mildly to Moderately Active Ulcerative Colitis:

• Adults: 800 mg (two 400 mg capsules) three times daily for 6 weeks.
• Pediatric Patients 5 years or older: See weight-based dosing table in the full prescribing information; twice daily dosing for 6 weeks.

Maintenance of Remission of Ulcerative Colitis:

• Adults: 1.6 grams (four 400 mg capsules) daily, in two to four divided doses.

Administration:

• Mesalamine comes as a delayed-release tablet, a delayed-release capsule, and an extended-release capsule to take by mouth.
• The delayed-release tablets (Lialda) are usually taken with food once a day by adults and children.
• The delayed-release tablets (Asacol HD) are usually taken on an empty stomach three times a day (1 hour before or 2 hours after meals) by adults.
• The extended-release capsules (Apriso) are usually taken with or without food once a day in the morning by adults.
• The extended-release capsules (Pentasa) are usually taken with or without food four times a day by adults.
• The extended-release capsules (Delzicol) are usually taken with or without food 2 to 4 times a day by adults and twice a day by children, preferably in the morning and afternoon.
• Swallow the delayed-release tablets, delayed-release capsules, and extended-release capsules whole; do not split, chew, or crush them.
• Be careful not to break the protective coating on the delayed-release tablets.
• If you cannot swallow the extended-release capsules (Pentasa), you may open the capsules and sprinkle the entire contents on a tablespoon of applesauce or yogurt.
• Swallow (without chewing) this mixture immediately after preparation. If you cannot swallow the delayed-release capsules (Delzicol), you may carefully open the capsules and swallow (without chewing) the entire contents of each capsule and then drink a glass of water to make sure you have swallowed all of the medicine.
• Drink plenty of fluids while taking mesalamine.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As a delayed-release tablet, a delayed-release capsule, and an extended-release capsule

This medicine is available in fallowing brand namesː

• Apriso; Asacol; Asacol HD; Delzicol; Lialda; Pentasa

What side effects can this medication cause?

The most common side effects of this medicine include:

• In Adults: eructation, abdominal pain, constipation, dizziness, rhinitis, back pain, and rash.
• In Pediatrics: nasopharyngitis, headache, abdominal pain, dizziness, sinusitis, rash, cough and diarrhea.

The most serious adverse reactions seen in mesalamine may include:

• Renal Impairment
• Mesalamine-Induced Acute Intolerance Syndrome
• Hypersensitivity Reactions
• Hepatic Failure
• Severe Cutaneous Adverse Reactions
• Photosensitivity
• Nephrolithiasis

What special precautions should I follow?

• Renal impairment, including minimal change disease, acute and chronic interstitial nephritis, and renal failure, has been reported in patients taking products such as mesalamine. Assess renal function at the beginning of treatment and periodically during treatment. Evaluate the risks and benefits of using mesalamine delayed-release capsules in patients with known renal impairment or taking nephrotoxic drugs; monitor renal function.
• Mesalamine has been associated with an acute intolerance syndrome that may be difficult to distinguish from an exacerbation of ulcerative colitis. Symptoms may be difficult to distinguish from an ulcerative colitis exacerbation; monitor for worsening symptoms while on treatment; discontinue treatment, if acute intolerance syndrome is suspected.
• Hypersensitivity reactions have been reported in patients taking sulfasalazine. Evaluate patients immediately and discontinue mesalamine delayed-release capsules, if a hypersensitivity reaction is suspected.
• There have been reports of hepatic failure in patients with pre-existing liver disease who have been administered mesalamine. Evaluate the risks and benefits of using mesalamine delayed-release capsules in patients with known liver impairment.
• Severe cutaneous adverse reactions, including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN), drug reaction with eosinophilia and systemic symptoms (DRESS), and acute generalized exanthematous pustulosis (AGEP) have been reported with the use of mesalamine. Discontinue at the first signs or symptoms of severe cutaneous adverse reactions or other signs of hypersensitivity and consider further evaluation.
• Patients treated with mesalamine or sulfasalazine who have pre-existing skin conditions such as atopic dermatitis and atopic eczema have reported more severe photosensitivity reactions. Advise patients with pre-existing skin conditions to avoid sun exposure, wear protective clothing, and use a broad-spectrum sunscreen when outdoors.
• Cases of nephrolithiasis have been reported with the use of mesalamine, including stones of 100% mesalamine content. Mesalamine-containing stones undetectable by standard radiography or computed tomography (CT). Ensure adequate fluid intake during treatment.
• Mesalamine delayed-release capsules contains iron oxide as a colorant in the coating of the delayed-release capsules. : Consider the iron content of mesalamine delayed-release capsules in patients taking iron supplementation and those at risk of iron overload.
• Use of mesalamine may lead to spuriously elevated test results when measuring urinary normetanephrine by liquid chromatography with electrochemical detection.
• Inform patients that if they are switching from a previous oral mesalamine therapy to mesalamine delayed-release capsules to discontinue their previous oral mesalamine therapy and follow the dosing instructions for mesalamine delayed-release capsules. Inform patients that two mesalamine delayed-release 400 mg capsules cannot be substituted for one mesalamine delayed-release 800 mg tablet.
• Mesalamine therapy has been associated with a low rate of serum enzyme elevations during therapy and with rare instances of clinically apparent acute liver injury.

What to do in case of emergency/overdose?

Symptoms of overdosage may 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.

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• 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 capsules is a pH dependent delayed-release product and this factor should be considered when treating a suspected overdose.

Can this medicine be used in pregnancy?

• There are no adequate and well controlled studies of mesalamine use in pregnant women.
• Mesalamine should be used during pregnancy only if clearly needed.

Can this medicine be used in children?

• The safety and effectiveness of mesalamine delayed-release capsules for the treatment of mildly to moderately active ulcerative colitis in pediatric patients 5 to 17 years of age has been established.
• The safety and effectiveness of mesalamine delayed-release capsules in the maintenance of remission of ulcerative colitis in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• MESALAMINE

Inactive ingredients:

• SILICON DIOXIDE
• DIBUTYL SEBACATE
• HYPROMELLOSE, UNSPECIFIED
• FERROSOFERRIC OXIDE
• FERRIC OXIDE RED
• LACTOSE MONOHYDRATE
• MAGNESIUM STEARATE
• METHACRYLIC ACID - METHYL METHACRYLATE COPOLYMER
• POLYETHYLENE GLYCOL 6000
• POTASSIUM HYDROXIDE
• POVIDONE K30
• PROPYLENE GLYCOL
• SHELLAC
• SODIUM STARCH GLYCOLATE TYPE A POTATO
• TALC

Who manufactures and distributes this medicine?

Manufactured In Israel By:

• Teva Pharmaceutical Ind. Ltd.
• Kfar Saba,, Israel

Manufactured For:

• Teva Pharmaceuticals USA, Inc.
• Parsippany, NJ

What should I know about storage and disposal of this medication?

• Store at 20º to 25ºC (68º to 77ºF).

• Dailymed label info on Mesalamine
• FDA Mesalamine

Mesalamine Resources
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