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Medications for IBD: Aminosalicylates

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Overview: Aminosalicylates do not suppress the immune system, so they reduce inflammation without decreasing the body’s ability to fight infection. They act locally on the bowel wall, so they produce less side effects. These are typically used as a first line therapy to treat mild disease due to their minimal side effects. They are much more effective in colitis vs Crohn’s, but can still play a role. 

 

Types: 

  • Mesalamine/mesalazine: anti-inflammatory drug similar to aspirin
    • Also referred to as 5-aminosalicylic acid or 5-ASA
    • Can be administered orally as a pill, as a suppository, or as an enema (liquid or foam)
    • Lots of different brand names and available in different controlled-release or delayed-release formulations
  • Source: Page 98 of Crohn’s and Colitis for Dummies 
Mesalamines 
Common Brand Name Formulation Use
Apriso Capsule Colitis
Asacol, Asacol HD Tablet Colitis
Cannasa Suppository Proctitis
Colazal Capsule Colitis
Dipentum Capsule Colitis
Delzicol Tablet Colitis
Lialda Tablet Colitis
Pentasa Capsule Colitis
Rowasa Suspension enema Proctosigmoiditis

 

Note: suppositories are inserted into the rectum where it dissolves or melts. They work locally and are especially helpful for proctitis or when you are unable to take anything by mouth. Nausea and pain medications are often given via suppository. 

  • Sulfasalazine: originally developed for rheumatoid arthritis
    • Common brand name is Azulfidine, given in tablet form for colitis 
    • Part of the class of drugs called sulfonamides and consists of a sulfa molecule connected to 5-ASA
    • The sulfa molecule was originally added for its antibacterial properties, but it has little effect on treating bowel inflammation
    • The drug acts like mesalamine, when the drug is broken down by the bacteria in the gut and the 5-ASA molecule is released 
    • It is prescribed less often because the addition of the sulfa molecule causes more side effects like nausea, vomiting, rash, and even anaphylaxis 

 

How do they work?

  • Inhibits inflammatory white blood cells and removes the free radicals that these cells produce 
  • Block the cell-to-cell signaling of inflammatory cells and their ability to move around the body 
  • Decrease tissue damage in the bowel and relieve symptoms 

 

When are they used?

  • More common in colitis than Crohn’s
  • Used to both induce and maintain remission of mild to moderate colitis 
  • Your doctor may use oral, rectal, or a combination of both treatments 
    • Oral treatment may be added if rectal treatments alone do not relieve symptoms or if inflammation involves a larger part of the colon and the rectal treatment cannot reach it.

 

Side effects: 

  • 5-ASA has mild side effects such as upset stomach and diarrhea, related to its local action
    • Kidney damage and pancreatitis are rare, your doctor will keep tabs on your kidney function 
    • About 3-5% of patients may experience worsening of symptoms and not be able to tolerate them 
  • Sulfasalazine may induce more symptoms:
    • Rash
    • Headache
    • Fatigue
    • Infertility in men (reversed if treatment is stopped)
    • Dangerous drop in white blood cell count (rare)

Notes: 

  • Those with sulfa allergy should avoid 
  • Inhibits the production of folic acid and you can develop folic acid deficiency and anemia 
    • Supplement with 1 mg/day minimum to prevent this