Asacol

Name: Asacol

Patient information

  • Instruct patients to swallow the Asacol tablets whole, taking care not to break, cut, or chew the tablets, because the coating is an important part of the delayed-release formulation.
  • Inform patients that if they are switching from a previous oral mesalamine therapy to Asacol they should discontinue their previous oral mesalamine therapy and follow the dosing instructions for Asacol. Inform patients that they should not substitute two Asacol 400 mg tablets with one Asacol HD 800 mg tablet [see DOSAGE AND ADMINISTRATION].
  • Inform patients that intact, partially intact, and/or tablet shells have been reported in the stool. Instruct patients to contact their physician if this occurs repeatedly.
  • Instruct patients to protect Asacol tablets from moisture. Instruct patients to close the container tightly and to leave any desiccant pouches present in the bottle along with the tablets.
  • Advise women who are pregnant, breastfeeding, or of childbearing potential that Asacol contains dibutyl phthalate, which was associated with malformations and adverse effects on the male reproductive system in animal studies. Dibutyl phthalate is excreted in human milk.

Uses of Asacol

Asacol is a prescription medication used to treat ulcerative colitis (UC). UC is a condition in which part or all of the lining of the colon (also known as the large intestine) is swollen or worn away. It is used to keep it from coming back ("maintain remission").

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Asacol and Lactation

Tell your doctor if you are breastfeeding or plan to breastfeed. The active ingredient in Asacol is excreted in human breast milk. The effect of Asacol on the nursing infant is not known.

 

What are some things I need to know or do while I take Asacol?

  • Tell all of your health care providers that you take this medicine. This includes your doctors, nurses, pharmacists, and dentists.
  • Avoid driving and doing other tasks or actions that call for you to be alert until you see how Asacol affects you.
  • Have blood work checked as you have been told by the doctor. Talk with the doctor.
  • This medicine may affect certain lab tests. Tell all of your health care providers and lab workers that you take this medicine.
  • You may get sunburned more easily. Avoid sun, sunlamps, and tanning beds. Use sunscreen and wear clothing and eyewear that protects you from the sun.
  • Some males have had sperm problems while taking Asacol. This may affect being able to father a child. This may go back to normal after the drug is stopped. Talk with the doctor.
  • Use with care in children. Talk with the doctor.
  • If you are 65 or older, use this medicine with care. You could have more side effects.
  • Do not give to children and teenagers who have or are getting better from flu signs, chickenpox, or other viral infections due to the chance of Reye's syndrome. Reye's syndrome causes very bad problems to the brain and liver.
  • You may see parts of Asacol in your stool. If this happens a lot, talk with your doctor.
  • Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using this medicine while you are pregnant.
  • Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

What are some side effects that I need to call my doctor about right away?

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.

Contraindications

Asacol is contraindicated in patients with known or suspected hypersensitivity to salicylates or aminosalicylates or to any of the ingredients of Asacol [see Warnings and Precautions (5.3), Adverse Reactions (6.2), and Description (11)].

Use in specific populations

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 1.9 times (rat) and 3.9 times (rabbit) the recommended human dose [see Data]. However, dibutyl phthalate (DBP) is an inactive ingredient in Asacol’s enteric coating, and in animal studies in rats at doses greater than 190 times the human dose, maternal DBP was associated with external and skeletal malformations and adverse effects on the reproductive system of male offspring. Advise pregnant women of the potential risk to the fetus.

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 2-4% and 15-20%, 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 impaired fertility or harm to the fetus. These mesalamine doses were about 1.9 times (rat) and 3.9 times (rabbit) the recommended human dose, based on body surface area.

DBP is an inactive ingredient in Asacol’s enteric coating. The human daily intake of DBP from the maximum recommended dose of Asacol tablets is about 21 mg. Published reports in rats show that male rat offspring exposed in utero to DBP (greater than or equal to 100 mg/kg/day, approximately 39 times the human dose based on body surface area), display reproductive system aberrations compatible with disruption of androgenic dependent development. The clinical significance of this finding in rats is unknown. At higher dosages (greater than or equal to 500 mg/kg/day, approximately 194 times the human dose based on body surface area), additional effects, including cryptorchidism, hypospadias, atrophy or agenesis of sex accessory organs, testicular injury, reduced daily sperm production, permanent retention of nipples, and decreased anogenital distance are noted. Female offspring are unaffected. High doses of DBP, administered to pregnant rats was associated with increased incidences of developmental abnormalities, such as cleft palate (greater than or equal to 630 mg/kg/day, about 244 times the human dose, based on body surface area) and skeletal abnormalities (greater than or equal to 750 mg/kg/day, about 290 times the human dose based on body surface area) in the offspring.

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. Additionally, DBP, an inactive ingredient in the enteric coating of Asacol tablets, and its primary metabolite mono-butyl phthalate (MBP) are present in human milk, but the clinical significance is unknown. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for Asacol and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition.

Clinical Considerations

Monitor breastfed infants for diarrhea.

Data

Human Data

In published lactation studies, maternal mesalamine doses from various oral and rectal formulations and products ranged from 500 mg to 3 g daily. The concentration of mesalamine in milk ranged from non-detectable to 0.11 mg/L. The concentration of the N-acetyl-5-aminosalicylic acid metabolite ranged from 5 to 18.1 mg/L. Based on these concentrations, estimated infant daily dosages for an exclusively breastfed infant are 0 to 0.017 mg/kg/day of mesalamine and 0.75 to 2.72 mg/kg/day of N-acetyl-5-aminosalicylic acid.

8.4 Pediatric Use

The safety and effectiveness of Asacol in pediatric patients 5 to 17 years of age for treatment of mildly to moderately active ulcerative colitis have been established over a 6-week period. Use of Asacol in these age groups is supported by evidence from adequate and well controlled studies of Asacol in adults and a single study in 82 pediatric patients 5 to 17 years of age [see Adverse Reactions (6.1), Clinical Pharmacology (12.3), and Clinical Studies (14.1)].

The safety and effectiveness of Asacol for the maintenance of remission of mildly to moderately active ulcerative colitis in pediatric patients have not been established. Efficacy was not demonstrated in a randomized, double-blind 26-week trial of two dosage levels for maintenance of remission of mildly to moderately active ulcerative colitis initiated in 39 patients aged 5 to 17 years. Possible factors contributing to this outcome included the dose range studied and premature termination of the trial. 

8.5 Geriatric Use

Clinical studies of Asacol did not include sufficient numbers of patients aged 65 and over to determine whether they respond differently than younger patients. Reports from uncontrolled clinical studies and postmarketing experience suggest a higher incidence of blood dyscrasias (agranulocytosis, neutropenia, pancytopenia) in patients receiving Asacol who are 65 years or older compared to younger patients. Monitor complete blood cell counts and platelet counts in elderly patients during treatment with Asacol. In general, the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy in elderly patients should be considered when prescribing Asacol [see Use in Specific Populations (8.6)].

8.6 Renal Impairment

Mesalamine is known to be substantially excreted by the kidney, and the risk of adverse reactions may be greater in patients with impaired renal function. Evaluate renal function in all patients prior to initiation and periodically while on Asacol therapy. Monitor patients with known renal impairment or history of renal disease or taking nephrotoxic drugs for decreased renal function and mesalamine-related adverse reactions [see Warnings and Precautions (5.1), Drug Interactions (7.1) and Adverse Reactions (6.2)].

References

  1. Turner D, Otley AR, Mack D, et al. Development, validation, and evaluation of a pediatric ulcerative colitis activity index: A prospective multicenter study. Gastroenterology. 2007;133:423–432.
  2. Schroeder KW, Tremaine WJ, Ilstrup DM. Coated oral 5-aminosalicylic acid therapy for mildly to moderately active ulcerative colitis. N Engl J Med. 1987;317(26):1625-9.

For the Consumer

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 Asacol) 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:

More common
  • Abdominal or stomach pain (severe)
  • bloody diarrhea
  • rectal bleeding
Less common
  • 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
Rare
  • 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:

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

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