In October, 2008 after getting the FDA approval, Salix Pharmaceuticals Company introduced its novel medication, called Apriso, to treat patients with ulcerative colitis (UC). Well, telling the truth, the medication is not “novel” in the full meaning of this word, because mesalamine, which is the main working ingredient of Apriso, is widely used today in other UC prescription medications, such as Pentasa, Rowasa, and Asacol; besides, it is also available in the generic form.
However, there is still one feature of Apriso, which grants an advantage to Apriso over the analogue medications. What is really new in Apriso is its unique combination of delayed and extended release technology of mesalamine delivery, which made Apriso the first and the only for the time being once-daily medication, indicated for the maintenance of ulcerative colitis (UC) remission in adults.
The point is that ulcerative colitis, which is a chronic inflammatory condition of the bowel, affects mainly colon or large intestine. And the main challenge for scientists is to deliver anti-inflammatory medication right to the affected area without having it destroyed by gastric acid in the stomach and small intestines. To reach this goal mesalamine medications (Asacol, Pentasa and others) are usually made in the form of delayed-release tablets, which start to dissolve only after passing the stomach.
Unlike its close rivals, Apriso features not only delayed-release technology, but the extended release as well. As the result of the prolonged and gradual release of its active ingredient, Apriso provides long-term effect on the colon, thus helping to keep ulcerative colitis symptoms in remission.
In general, the pattern of Apriso mode of action is as follows:
- first, the medication gel outer layer is dissolved in the stomach and the microgranules with the active ingredient are dispersed into digestive tract;
- then the coating of the microgranules starts to dissolve at pH 6.0 or higher and the release of mesalamine begins; - the particular level of pH is used to “tell” the medication that it has already reached the colon and it is time to start working (by the way, it is said that other analogue medications start to dissolve only at pH 7.0 or higher, while many people never reach that level of pH in their large intestine);
- finally, the special polymer matrix core of Apriso controls the extended release of mesalamine to provide the distribution of main working substance throughout all the affected areas.
As the result of new delivery mechanism implementation patients can take Apriso only once per whole day (in the amount of 1.5 g, which is 4 capsules), usually in the morning with or without food. For comparison, Asacol is usually taken 3 times a day, and Pentasa is recommended twice a day.
So, from the point of view of users’ convenience only Lialda (another recently approved once-day UC treatment) may compete with Apriso. However, the recommended dosage of Lialda is 2.4 g per day versus 1.5 g of Apriso. On one hand, this may translate into lower side effects associated with Apriso, but on the other hand it may also mean lower effectiveness.
Anyway, since the working ingredient is the same in all the mentioned medications, it may only be a matter of trying different products to define the one, which suits your therapeutic expectations best.
P.S. Taking Apriso along with antacids is not the best idea, because antacids influence pH level, which may bring to nothing all the efforts of highly-sophisticated Apriso technology of delivering mesalamine right where it is needed.
You have made a lot of poor points in your article. Apriso is NOT the ONLY once daily mesalamine on the market. Lialda, the FIRST ONCE-A-DAY medication, which came out over 3 year ago is far superior to Apriso. Most doctors will tell you that they find 1500mg or 1.5g of mesalamine sub-therapeutic, which means they believe that is not enough mesalamine to keep a person from actively flaring. Doctors recommend at LEAST 2400mg or 2.4g a day! Secondly, a patient has to take a MINIMUM of 4 pills once daily of Apriso to even get 1500 mg; a patient only has to take 2 pills once daily of lialda to get 2400mg or 2.4g of mesalamine! Also, Apriso is only indicated by the FDA for the MAINTENANCE of remission in mild to moderate UC patients. This means that if a patient who has ACTIVE UC (means active diarhea or bleeding)takes Apriso, they are taking a drug that has never been proven to work on patients who are actively flaring - Apriso has only been proven to work on patients that have been in remission. Lialda, on the other hand, is indicated by the FDA to INDUCE remission in mild to moderate UC patients - meaning that if a patient who is actively flaring takes a prescribed 2400mg or 4800mg of Lialda, this drug has been shown to bring a patient out of a flare and into remission. Lastly, you discuss the mechanism of action of Apriso as if much of the drug actually gets to the colon! UC is a surface drug that doesn't even start until the colon. A patient can't have UC of the small intestine. Sooo....why would a we want to take a tablet, like Apriso, that starts releasing mesalamine (the active drug) into our small intestine? Not to mention, I've read that 33% of Apriso is ABSORBED in the small intestine! UC is a SURFACE disease, meaning it doesn't affect all of the various layers of the mucosal wall. So absorption is a BAD THING! This absorption from the Apriso pill, also means that LESS THAN 1gram of mesalamine is even getting to the colon at all!! And I stated earlier that doctors believe anything under 2.4g of mesalmine won't help a patient achieve remission! Lialda, on the other hand, is PH-dependent and starts releasing the medication at a ph of 7, which never, no matter what, occurs until our colons! This means you CAN take antacids with Lialda, just FYI.
I appreciate you trying to alert us patients to a "new" drug, but make sure you are giving us CORRECT information! Thanks
Lialda never did. If you can go for Lialda!!!