Pentasa

Pentasa is a prescription medication used to treat ulcerative colitis, or inflammation of the lining of the colon. It helps relieve the symptoms of ulcerative colitis including diarrhea, rectal bleeding, and stomach pain. Pentasa belongs to a group of drugs called aminosalicylates. These work by stopping the body from producing a certain substance that may cause pain or inflammation in the colon.

Pentasa is available as capsules and are usually taken taken up to 4 times a day, with or without food.

Common side effects of Pentasa include diarrhea, headache, and nausea.

Pentasa is part of the drug class:

• Aminosalicylic acid and similar agents

If you take too much this medication, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

• If you have an allergy to mesalamine, salicylates, sulfasalazine, or any other part of Pentasa (mesalamine long-acting capsules (pentasa)).
• If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
• If you have any of these health problems: Kidney disease or liver disease.
• If you have had the varicella vaccine in the past 6 weeks.

This is not a list of all drugs or health problems that interact with this medicine.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take Pentasa with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Signs of liver problems like dark urine, feeling tired, not hungry, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes.
• Signs of kidney problems like unable to pass urine, change in how much urine is passed, blood in the urine, or a big weight gain.
• Chest pain or pressure.
• Throwing up blood or throw up that looks like coffee grounds.
• A burning, numbness, or tingling feeling that is not normal.
• Feeling confused.
• A fast heartbeat.
• A heartbeat that does not feel normal.
• Fever or chills.
• Very bad headache.
• Very bad dizziness.
• Very bad back pain.
• Shortness of breath, a big weight gain, or swelling in the arms or legs.
• Any unexplained bruising or bleeding.
• Feeling very tired or weak.
• Some people may have a reaction to this medicine that looks like the signs of ulcerative colitis. Call your doctor right away if you have very bad belly pain or cramps, bloody stools, fever, headache, or rash.

• Store at room temperature.
• Store in a dry place. Do not store in a bathroom.
• Protect from light.
• Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
• Check with your pharmacist about how to throw out unused drugs.

• If your symptoms or health problems do not get better or if they become worse, call your doctor.
• Do not share your drugs with others and do not take anyone else's drugs.
• Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.
• Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.
• Some drugs may have another patient information leaflet. Check with your pharmacist. If you have any questions about Pentasa (mesalamine long-acting capsules (pentasa)), please talk with your doctor, nurse, pharmacist, or other health care provider.
• If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about Pentasa. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using Pentasa.

Review Date: October 4, 2017

Pentasa (mesalamine) for oral administration is a controlled-release formulation of mesalamine, an aminosalicylate anti-inflammatory agent for gastrointestinal use.

Chemically, mesalamine is 5-amino-2-hydroxybenzoic acid. It has a molecular weight of 153.14.

The structural formula is:

Each 250 mg capsule contains 250 mg of mesalamine. It also contains the following inactive ingredients: acetylated monoglyceride, castor oil, colloidal silicon dioxide, ethylcellulose, hydroxypropyl methylcellulose, starch, stearic acid, sugar, talc, and white wax. The capsule shell contains D&C Yellow #10, FD&C Blue #1, FD&C Green #3, gelatin, titanium dioxide, and other ingredients.

Each 500 mg capsule contains 500 mg of mesalamine. It also contains the following inactive ingredients: acetylated monoglyceride, castor oil, colloidal silicon dioxide, ethylcellulose, hydroxypropyl methylcellulose, starch, stearic acid, sugar, talc, and white wax. The capsule shell contains FD&C Blue #1, gelatin, titanium dioxide, and other ingredients.

Sulfasalazine is split by bacterial action in the colon into sulfapyridine (SP) and mesalamine (5-ASA). It is thought that the mesalamine component is therapeutically active in ulcerative colitis. The usual oral dose of sulfasalazine for active ulcerative colitis in adults is 2 to 4 g per day in divided doses. Four grams of sulfasalazine provide 1.6 g of free mesalamine to the colon.

The mechanism of action of mesalamine (and sulfasalazine) is unknown, but appears to be topical rather than systemic. Mucosal production of arachidonic acid (AA) metabolites, both through the cyclooxygenase pathways, ie, prostanoids, and through the lipoxygenase pathways, ie, leukotrienes (LTs) and hydroxyeicosatetraenoic acids (HETEs), is increased in patients with chronic inflammatory bowel disease, and it is possible that mesalamine diminishes inflammation by blocking cyclooxygenase and inhibiting prostaglandin (PG) production in the colon.

Human Pharmacokinetics and Metabolism
Absorption. Pentasa is an ethylcellulose-coated, controlled-release formulation of mesalamine designed to release therapeutic quantities of mesalamine throughout the gastrointestinal tract. Based on urinary excretion data, 20% to 30% of the mesalamine in Pentasa is absorbed. In contrast, when mesalamine is administered orally as an unformulated 1-g aqueous suspension, mesalamine is approximately 80% absorbed.

Plasma mesalamine concentration peaked at approximately 1 μg/mL 3 hours following a 1-g Pentasa dose and declined in a biphasic manner. The literature describes a mean terminal half-life of 42 minutes for mesalamine following intravenous administration. Because of the continuous release and absorption of mesalamine from Pentasa throughout the gastrointestinal tract, the true elimination half-life cannot be determined after oral administration. N-acetylmesalamine, the major metabolite of mesalamine, peaked at approximately 3 hours at 1.8 μg/mL, and its concentration followed a biphasic decline. Pharmacological activities of N-acetylmesalamine are unknown, and other metabolites have not been identified.

Oral mesalamine pharmacokinetics were nonlinear when Pentasa capsules were dosed from 250 mg to 1 g four times daily, with steady-state mesalamine plasma concentrations increasing about nine times, from 0.14 μg/mL to 1.21 μg/mL, suggesting saturable first-pass metabolism. N-acetylmesalamine pharmacokinetics were linear.

Elimination. About 130 mg free mesalamine was recovered in the feces following a single 1-g Pentasa dose, which was comparable to the 140 mg of mesalamine recovered from the molar equivalent sulfasalazine tablet dose of 2.5 g. Elimination of free mesalamine and salicylates in feces increased proportionately with Pentasa dose. N-acetylmesalamine was the primary compound excreted in the urine (19% to 30%) following Pentasa dosing.

191-08
NDC 54092-191-08

Pentasa®
(mesalamine)

Controlled-Release Capsules

8 CAPSULES

Rx only

Patient Sample–Not for Sale

500 mg

Shire

Applies to mesalamine: oral capsule delayed release, oral capsule extended release, oral tablet, oral tablet delayed release, oral tablet enteric coated

Other dosage forms:

• rectal enema, rectal suppository

Along with its needed effects, mesalamine (the active ingredient contained in Pentasa) may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur while taking mesalamine:

• Abdominal or stomach pain (severe)
• bloody diarrhea
• rectal bleeding

• Abdominal or stomach cramps (severe)
• blurred vision
• dizziness
• fever
• full or bloated feeling
• headache (severe)
• nervousness
• pounding in the ears
• pressure in the stomach
• skin rash and itching
• slow or fast heartbeat
• swelling of the abdominal or stomach area
• unusual tiredness or weakness

• Anxiety
• back pain (severe)
• blue or pale skin
• chest pain, possibly moving to the left arm, neck, or shoulder
• chills
• nausea or vomiting
• yellow eyes or skin

Some side effects of mesalamine may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

• Abdominal or stomach cramps or pain (mild)
• diarrhea (mild)
• headache (mild)
• runny or stuffy nose
• sneezing

• Acid or sour stomach
• acne
• back or joint pain
• belching
• difficulty with moving
• excess air or gas in the stomach or intestines
• hair loss or thinning of the hair
• heartburn
• indigestion
• loss of appetite
• muscle pain or stiffness
• passing gas
• stomach discomfort or upset