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About 5-ASA / Mesalazine / Pentasa / Asacol / Lialda and Like Formulations

David

Co-Founder
Staff member
Location
Naples, Florida
Mesalazine (5-ASA) is an anti-inflammatory drug used to treat inflammation of the digestive tract for people with mild-to-moderate Crohn's Disease and Ulcerative Colitis.

Formulations

Mesalazine has many different formulations with different brand names. Please note that the various formulations are usually slightly different in how they target inflammation. Some of those names are:

US: Canasa, Rowasa, Pentasa, Asacol, Lialda, Apriso, Colazal
UK: Asacol, Ipocal, Pentasa, Salofalk, Mezavant XL
France: Asacol, Pentasa, Mezavant
Canada: Asacol, Pentasa, Salofalk, Mezavant
Mexico: Salofalk
Australia: Mesasal, Pentasa, Salofalk

Potential Side Effects

Some of the potential side effects include: Diarrhea, nausea, cramping, flatulence, headache, exacerbation of the colitis, hypersensitivity reactions (including rash, urticaria aka hives, interstitial nephritis and lupus erythematosus-like syndrome), hair loss, and [wiki]interstitial nephritis[/wiki], acute pancreatitis, hepatitis, nephrotic syndrome, blood disorders (including agranulocytosis, aplastic anaemia, leukopenia, neutropenia, thrombocytopenia), allergic lung reaction, allergic myocarditis, methaemoglobinaemia.

This thread is meant to be collaboratively improved over time. If you have information to add or corrects to be made, please respond to this thread with the pertinent info and, if possible, a quality reference for that information.

Check out the CrohnsForum Wiki Page for Mesalamine [wiki=Mesalamine]HERE[/wiki]
 
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Well i've been on 4g of 5-ASA ( Salofalk 500mg) eversince my diagnosis in june. and i've noticed non of these side effects mentioned other than increase in acne- the really swollen type, tho i did notice that it gave me gas, and a whole lot of it and i do seem to catch colds easier than before like every other week i get a massive headache n fever- unfortunately timed perfectly before the weekend, given that the past 5 yrs i havent caught a single cold.
 

DustyKat

Super Moderator
5-ASA (mesalamine) oral medications

5-aminosalicylic acid (5-ASA), also called mesalamine, is similar chemically to aspirin. Aspirin is an anti-inflammatory drug that has been used for many years for treating arthritis, bursitis, and tendonitis (conditions of tissue inflammation). Aspirin, however, is not effective in treating Crohn's disease and ulcerative colitis, and even may worsen the inflammation. Aspirin, however, is not effective in treating Crohn's disease and ulcerative colitis and may even worsen the inflammation. Recent studies suggest that aspirin might actually decrease future risk of developing colorectal cancer in the general population.

On the other hand, 5-ASA can be effective in treating Crohn's disease and ulcerative colitis if the drug can be delivered topically onto the inflamed intestinal lining. For example, mesalamine (Rowasa) is an enema containing 5-ASA that is effective in treating inflammation in the rectum. However, the enema solution cannot reach high enough to treat inflammation in the upper colon and the small intestine. Therefore, for most patients with Crohn's disease involving both the ileum (distal small intestine) and colon, 5-ASA must be taken orally.

If pure 5-ASA is taken orally, however, most of the 5-ASA would be absorbed in the stomach and the upper small intestine, and very little 5-ASA would reach the ileum and colon. To be effective as an oral agent in treating Crohn's disease, 5-ASA has to be modified chemically to escape absorption by the stomach and the upper intestines.

Sulfasalazine (Azulfidine)

Sulfasalazine (Azulfidine) was the first modified 5-ASA compound used in the treatment of Crohn's colitis and ulcerative colitis. It has been used successfully for many years to induce remissions among patients with mild to moderate ulcerative colitis. Sulfasalazine also has been used for prolonged periods for maintaining remissions.

Sulfasalazine consists of a 5-ASA molecule linked chemically to a sulfapyridine molecule. (Sulfapyridine is a sulfa antibiotic.) Connecting the two molecules together prevents absorption by the stomach and the upper intestines. When sulfasalazine reaches the ileum and the colon, the bacteria that normally are present in the ilium and colon break the link between the two molecules. After breaking away from 5-ASA, sulfapyridine is absorbed into the body and later eliminated in the urine. Most of the active 5-ASA, however, is available within the terminal ileum and colon to treat the colitis.

Most of the side effects of sulfasalazine are due to the sulfapyridine molecule. These side effects include nausea, heartburn, headache, anemia, skin rashes, and, in rare instances, hepatitis and kidney inflammation. In men, sulfasalazine can reduce the sperm count. The reduction in sperm count is reversible, and the count usually becomes normal after the sulfasalazine is discontinued or changed to a different 5- ASA compound.

Because the newer 5-ASA compounds, for example, mesalamine (Asacol and Pentasa), do not have the sulfapyridine component and have fewer side effects than sulfasalazine, they are being used more frequently for treating Crohn's disease and ulcerative colitis.

Asacol

Asacol is a tablet consisting of the 5-ASA compound surrounded by an acrylic resin coating. Asacol is sulfa-free. The resin coating prevents the 5-ASA from being absorbed as it passes through the stomach and the small intestine. When the tablet reaches the terminal ileum and the colon, the resin coating dissolves, and the active 5-ASA drug is released.

Asacol is effective in inducing remissions in patients with mild to moderate ulcerative colitis. It also is effective when used in the longer term to maintain remissions. Some studies have shown that Asacol also is effective in treating Crohn's ileitis and ileo-colitis, as well as in maintaining remission in patients with Crohn's disease.

The recommended dose of Asacol for inducing remissions is two 400 mg tablets three times daily (a total of 2.4 grams a day). At least two tablets of Asacol twice daily (1.6 grams a day) is recommended for maintaining remission. Occasionally, the maintenance dose is higher.

As with Azulfidine, the benefits of Asacol are dose-related. If patients do not respond to 2.4 grams a day of Asacol, the dose frequently is increased to 3.6 - 4.8 grams a day to induce remission. If patients fail to respond to the higher doses of Asacol, then other alternatives such as corticosteroids are considered.

Pentasa

Pentasa is a capsule consisting of small spheres containing 5-ASA. Pentasa is sulfa-free. As the capsule travels down the intestines, the 5-ASA inside the spheres is released slowly into the intestine. Unlike Asacol, the active drug 5-ASA in Pentasa is released into the small intestine as well as the colon. Therefore, Pentasa can be effective in treating inflammation in the small intestine and is currently the most commonly used 5-ASA compound for treating mild to moderate Crohn's disease in the small intestine.

Patients with Crohn's disease occasionally undergo surgery to relieve small intestinal obstruction, drain abscesses, or remove fistulae. Usually, the diseased portions of the intestines are removed during surgery. After successful surgery, patients can be free of disease and symptoms (in remission) for a while. In many patients, however, Crohn's disease eventually returns. Pentasa helps maintain remissions and reduces the chances of the recurrence of Crohn's disease after surgery.

In the treatment of Crohn's ileitis or ileocolitis, the dose of Pentasa usually is four 250 mg capsules four times daily (a total of 4 grams a day). For maintenance of remission in patients after surgery, the dose of Pentasa is between 3-4 grams daily.

Olsalazine (Dipentum)

Olsalazine (Dipentum) is a capsule filled with a drug in which two molecules of 5-ASA are joined together by a chemical bond. In this form, the 5-ASA cannot be absorbed from the stomach and intestine. Intestinal bacteria are able to break apart the two molecules releasing the active individual 5-ASA molecules into the intestine. Since intestinal bacteria are more abundant in the ileum and colon, most of the active 5-ASA is released in these areas. Therefore, olsalazine is most effective for disease that is limited to the ileum or colon. Although clinical studies have shown that olsalazine is effective for maintenance of remission in ulcerative colitis, up to 11% of patients experience diarrhea when taking olsalazine. Because of this, olsalazine is not often used. The recommended dose of olsalazine is 500 mg twice a day.

Balsalazide (Colazal)

Balsalazide (Colazal) is a capsule in which the 5-ASA is linked by a chemical bond to another molecule that is inert (without effect on the intestine) and prevents the 5-ASA from being absorbed. This drug is able to travel through the intestine unchanged until it reaches the end of the small bowel (terminal ileum) and colon. There, intestinal bacteria split the 5-ASA and the inert molecule releasing the 5-ASA. Because intestinal bacteria are most abundant in the terminal ileum and colon, balsalazide is used to treat inflammation predominantly localized to the colon.

Side effects of oral 5-ASA compounds

The 5-ASA compounds have fewer side effects than Azulfidine and also do not reduce sperm counts. They are safe medications for long-term use and are well-tolerated.

Patients allergic to aspirin should avoid 5-ASA compounds because they are similar chemically to aspirin.

Rare kidney and lung inflammation has been reported with the use of 5-ASA compounds. Therefore, 5-ASA should be used with caution in patients with kidney disease. It also is recommended that blood tests of kidney function be done before starting and periodically during treatment.

Rare instances of worsening of diarrhea, cramps, and abdominal pain, at times accompanied by fever, rash, and malaise, may occur. This reaction is believed to represent an allergy to the 5-ASA compound.

http://www.medicinenet.com/crohns_disease/page6.htm

Dusty. :)
 

DustyKat

Super Moderator
5-ASA rectal medications (Rowasa Canasa)

Rowasa is 5-ASA in enema form. 5-ASA by enema is most useful for treating ulcerative colitis involving only the distal colon since the enema easily can reach the inflamed tissues of the distal colon. Rowasa also is used in treating Crohn's disease in which there is inflammation in and near the rectum. Each Rowasa enema contains 4 grams of 5-ASA. The enema usually is administered at bedtime, and patients are encouraged to retain the enema through the night. The enema contains sulfite and should not be used by patients with sulfite allergy. Otherwise, Rowasa enemas are safe and well-tolerated.

Canasa is 5-ASA in suppository form. It is used for treating ulcerative proctitis. Each suppository contains 500 mg of 5-ASA and usually is administered twice daily.

Both enemas and suppositories have been shown to be effective in maintaining remission in patients with ulcerative colitis limited to the distal colon and rectum.

http://www.medicinenet.com/crohns_disease/page7.htm

Dusty. :)
 

Kev

Senior Member
OK. I've taken 4G of 5-ASA for the past 7 years. But, I recently noticed a major change in my health, and as a precaution, the 5-ASA has been discontinued. Turns out, on top of my Crohns, I now have Diabetes to contend with. Now, no one is pointing a finger per se at 5-ASA, but on the off chance that it was/is affecting my pancreas, it was taken off the table. (so to speak). If my insulin levels stabilize/increase over the next 8 - 12 weeks, then we've nailed the culprit. If they don't, it doesn't eliminate the very remote tho possibly real issue that 5-ASA may be the cause. Of course, it could also be age, gender, genes, Crohns, or other related issues.... I'm hoping that it is/was the 5-ASA, and that removing it will allow this to all just go away. But I'm not betting the bank.

As a side note, any other Crohnies out there who also are Diabetic? Drop me a line, OK?
 
David,
Don't forget to add in your list of medications that Delzicol has replaced Asacol. You can also add Asacol HD to the list.
 
Okay so just yesterday 5/15/13 i was told i have crohns and have been given Lialda (mesalamine) to take. Im not a huge fan of taking meds..u was told i have to take this everyday for the rest of my life. Is this true? Cant i just take it as needed?

Jim
 
Jim,
There are times that I have felt just like you do about meds. However, there presently is no cure for Crohn's Disease and your symptoms could come back or get worse if you don't take your medicine. Most people don't have problems with Lialda.
 
The meds will help you stay in remission. If you slack off on taking them, you most likely will experience another flareup and the diarrhea and pain associated with it. And it then takes longer to get back in remission. If the meds work for you, take them and count your blessings.
 
In India the generic equivalent of Asacol (by Tillotts) called Mesacol (by sun pharma) is being promoted by the govt though private practitioners are reluctance to prescribe this guess due to the commissions. doctors of Hospitals run on nonprofit do prescribe mesacol Mesacol is around 1/3 the price of asacol.

I was on asacol and sometimes when asacol was not available i would buy a strip of Mesacol, Asacol has to be specially ordered in most pharmacies. Now with the small change and stopping of asacol I am confused abt what small difference is there in Mesacol and asacol.
 
In Canada, Salofalk is available in tablets and rectal enemas. I have been on both for just over 3 years. 3,000 mg of tablets per day and one 4g enema every other day, although if I start to flare, I can up my dosage to 6,000 mg of tablets and 4g enema every day. I have noticed fatigue, gas and skin rashes as side effects; however all are tolerable considering I mostly have a normal life now except during the mornings after first food of the day. I also take 1/2 package of Cholorestryne daily in the morning. For now, things are pretty good. We all have to get used to a new kind of normal once we are diagnosed with C or UC.

I was on Asacol at the beginning but the tablets were going right through me, Salofalk tablets apparently dissolved differently.
 
I was diagnosed with UC last October and have been on Mesalamine enemas, once at night and just recently started Apriso. I find that this particular medicine causes vertigo like symptoms. I am also finding that the meds are not working for me even after a couple rounds of steroids. I am off gluten due to having celiacs but really everything I eat causes pain and goes through me. I find myself not eating until I am at home. Very frustrating and want to try an alternative method to see if I can stop the meds. Any advice, comments?
 
I always chuckle when i read the side effects for my meds and see things like 'diarhoea' and 'abdominal pain' etc. Makes you wonder why you're even taking the drugs lol.
 
I already have crohns , do I really need other health issues while taking these meds? Eat right excersise , smoke a joint .
 

DustyKat

Super Moderator
It is good to hear that works for you Bonzo and long may that be the case. :)

Unfortunately for others it isn’t enough and it is not for want of trying. :(
 
I always chuckle when i read the side effects for my meds and see things like 'diarhoea' and 'abdominal pain' etc. Makes you wonder why you're even taking the drugs lol.
My thoughts exactly !!! :eek2: I freaked when I read all the possible side effects of Mesalamine (Apriso) my GI just started me on. Geeeeeesh. Better NOT be the case!
So far, so good, though. On day three and so far just some mild vertigo and some crazy back itch along with occasional back pain. We'll see if anything else develops. Hope not.
 
I started Pentasa tablets and Salofalk suppositories on Tuesday afternoon (it's now Saturday). Yesterday I had my first blood-free (that I could see) BM since mid-February. I've been almost completely pain-free today as well. Of course every person is different, so your experience may well be different, but hopefully not too long!
 
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I was put on Lliada recently. I was told to take it in the morning. The last couple of days it has been in the afternoon. Does that make a difference?

2
 
My son was recently diagnosed with non-specific ulcers in the mid-portion of the small bowel. They may be an indication of early Crohns based on my history (diagnosed in 1977). First prescribed Pentasa but declined by our insurance formulary so approved for Lialda. I'm really wondering if it will help since every thing I've read says it's absorbed in the colon and I also wonder if he should take 5-ASAs without a definitive CD diagnosis. He had the Pill Cam which I thought was able to provide a correct diagnosis. He's suffered with symptoms for almost five years now. Any help/advice would be greatly appreciated. Thank you.
 
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Anyone taking 6 pentasa a day (each is 500mg) ? And 20 mg omeprazole ? I have terrible Heartburn recently after taking 6 pentasa a day. What should I do ?
 
Hi Ozman
Do you take your pentasa at the end of a meal? That makes a big difference. I don't know what you were recommended, I take half my daily dose after breakfast and half after my evening meal.
I don't know how long you have been taking them, it might take your body a while to get used to them.
 
Hi Ozman
Do you take your pentasa at the end of a meal? That makes a big difference. I don't know what you were recommended, I take half my daily dose after breakfast and half after my evening meal.
I don't know how long you have been taking them, it might take your body a while to get used to them.
Battling crohns disease for 4 years, first 3 years I had no flares no symptoms, took Pentasa Imuran with no issues, life was awesome, this year my calprotectin went outrageous, too much weightloss, joint ache, so for time being my doctor increased my pentasa from 4 tabs to 6 tabs a day, started taking pentomax (omeprazole) as well. Yea I take pentasa after meal. But dealing with very dry mouth, Heartburn & too much swallowing difficulty. All these symptoms gradually started (not in 1 day or week). Went to ENT for my restless jaw & swallowing issues, he said my throat looks fine :( I recently have symptoms of TMJ :'( Oh forgot to mention my allergies is super high (IgE is 150+ units). Can't take allergy meds cause of too dry mouth. I am super depressed .
 
We are the same here! I tend to just make sure they eat fruit and veg, I'm afraid I rarely seem to be organised enough to try new recipes, etc. We have a juicer so I try make a veg juice most days
Battling crohns disease for 4 years, first 3 years I had no flares no symptoms, took Pentasa Imuran with no issues, life was awesome, this year my calprotectin went outrageous, too much weightloss, joint ache, so for time being my doctor increased my pentasa from 4 tabs to 6 tabs a day, started taking pentomax (omeprazole) as well. Yea I take pentasa after meal. But dealing with very dry mouth, Heartburn & too much swallowing difficulty. All these symptoms gradually started (not in 1 day or week). Went to ENT for my restless jaw & swallowing issues, he said my throat looks fine :( I recently have symptoms of TMJ :'( Oh forgot to mention my allergies is super high (IgE is 150+ units). Can't take allergy meds cause of too dry mouth. I am super depressed .
I am sorry for what you are going through.
 
Ozman, are you sure the IgE is due to food allergies? The most obvious causes would be allergies such as house dust mite/pollen/animal hair.
 
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