Olsalazine

Last updated
Olsalazine
Olsalazine.svg
Clinical data
Trade names Dipentum
AHFS/Drugs.com Monograph
MedlinePlus a601088
License data
Pregnancy
category
Routes of
administration
By mouth
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: ℞-only
Pharmacokinetic data
Protein binding 99%
Elimination half-life 0.9 hours
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.116.494 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C14H10N2O6
Molar mass 302.242 g·mol−1
3D model (JSmol)
  • O=C(O)c1cc(ccc1O)/N=N/c2cc(C(O)=O)c(O)cc2
  • InChI=1S/C14H10N2O6/c17-11-3-1-7(5-9(11)13(19)20)15-16-8-2-4-12(18)10(6-8)14(21)22/h1-6,17-18H,(H,19,20)(H,21,22)/b16-15+ Yes check.svgY
  • Key:QQBDLJCYGRGAKP-FOCLMDBBSA-N Yes check.svgY
 X mark.svgNYes check.svgY  (what is this?)    (verify)

Olsalazine is an anti-inflammatory medication used in the treatment of ulcerative colitis. [2] [3] It is sold under the brand name Dipentum. [4]

Contents

Olsalazine itself is a pro-drug of mesalazine (5-aminosalicyclic acid or 5-ASA) and is not absorbed in the small intestine. Instead it continues through to the colon where it is cleaved into two molecules of 5-ASA by azoreductases produced by colonic bacteria. Olsalazine thus exerts its anti-inflammatory effect by its colonic breakdown into 5-ASA which inhibits cyclooxygenase and lipoxygenase thereby reducing prostaglandin and leukotriene production. [4]

History

Olsalazine gained Food and Drug Administration (FDA) approval in 1990.

Supply

The drug is supplied by UCB Pharma.

Research

In 2006 the Australian biotech company Giaconda received a European patent for a combination therapy for treating constipation-predominant irritable bowel syndrome that uses olsalazine and the anti-gout drug colchicine, for trials the following year. [5]

Related Research Articles

<span class="mw-page-title-main">Crohn's disease</span> Type of inflammatory bowel disease

Crohn's disease is a type of inflammatory bowel disease (IBD) that may affect any segment of the gastrointestinal tract. Symptoms often include abdominal pain, diarrhea, fever, abdominal distension, and weight loss. Complications outside of the gastrointestinal tract may include anemia, skin rashes, arthritis, inflammation of the eye, and fatigue. The skin rashes may be due to infections as well as pyoderma gangrenosum or erythema nodosum. Bowel obstruction may occur as a complication of chronic inflammation, and those with the disease are at greater risk of colon cancer and small bowel cancer.

<span class="mw-page-title-main">Ulcerative colitis</span> Inflammatory bowel disease that causes ulcers in the colon

Ulcerative colitis (UC) is one of the two types of inflammatory bowel disease (IBD), with the other type being Crohn's disease. It is a long-term condition that results in inflammation and ulcers of the colon and rectum. The primary symptoms of active disease are abdominal pain and diarrhea mixed with blood (hematochezia). Weight loss, fever, and anemia may also occur. Often, symptoms come on slowly and can range from mild to severe. Symptoms typically occur intermittently with periods of no symptoms between flares. Complications may include abnormal dilation of the colon (megacolon), inflammation of the eye, joints, or liver, and colon cancer.

<span class="mw-page-title-main">Infliximab</span> Biopharmaceutical drug for autommune disorders

Infliximab, a chimeric monoclonal antibody, sold under the brand name Remicade among others, is a medication used to treat a number of autoimmune diseases. This includes Crohn's disease, ulcerative colitis, rheumatoid arthritis, ankylosing spondylitis, psoriasis, psoriatic arthritis, and Behçet's disease. It is given by slow injection into a vein, typically at six- to eight-week intervals.

<span class="mw-page-title-main">Inflammatory bowel disease</span> Medical condition

Inflammatory bowel disease (IBD) is a group of inflammatory conditions of the colon and small intestine, with Crohn's disease and ulcerative colitis (UC) being the principal types. Crohn's disease affects the small intestine and large intestine, as well as the mouth, esophagus, stomach and the anus, whereas UC primarily affects the colon and the rectum.

<span class="mw-page-title-main">Colitis</span> Inflammation of the colon (large intestine)

Colitis is swelling or inflammation of the large intestine (colon). Colitis may be acute and self-limited or long-term. It broadly fits into the category of digestive diseases.

<span class="mw-page-title-main">Mesalazine</span> Anti-inflammatory medication

Mesalazine, also known as mesalamine or 5-aminosalicylic acid (5-ASA), is a medication used to treat inflammatory bowel disease, including ulcerative colitis and Crohn's disease. It is generally used for mildly to moderately severe disease. It is taken by mouth or rectally. The formulations which are taken by mouth appear to be similarly-effective.

<span class="mw-page-title-main">Sulfasalazine</span> Chemical compound

Sulfasalazine, sold under the brand name Azulfidine among others, is a medication used to treat rheumatoid arthritis, ulcerative colitis, and Crohn's disease. It is considered by some to be a first-line treatment in rheumatoid arthritis. It is taken by mouth or can be administered rectally.

<span class="mw-page-title-main">Colectomy</span> Surgical removal of any extent of the colon

Colectomy is bowel resection of the large bowel (colon). It consists of the surgical removal of any extent of the colon, usually segmental resection. In extreme cases where the entire large intestine is removed, it is called total colectomy, and proctocolectomy denotes that the rectum is included.

<span class="mw-page-title-main">4-Aminosalicylic acid</span> Anti-tuberculosis and anti-inflammatory drug

4-Aminosalicylic acid, also known as para-aminosalicylic acid (PAS) and sold under the brand name Paser among others, is an antibiotic primarily used to treat tuberculosis. Specifically it is used to treat active drug resistant tuberculosis together with other antituberculosis medications. It has also been used as a second line agent to sulfasalazine in people with inflammatory bowel disease such as ulcerative colitis and Crohn's disease. It is typically taken by mouth.

<span class="mw-page-title-main">Collagenous colitis</span> Medical condition

Collagenous colitis is an inflammatory condition of the colon. Together with the related condition lymphocytic colitis, it is a subtype of microscopic colitis, which is characterized by inflammation that specifically affects the colon, and a clinical presentation that involves watery diarrhea but a lack of rectal bleeding. Microscopic colitis does not usually cause macroscopic changes to the colon that allow a visual diagnosis during colonoscopy, instead causing microscopic changes that can be detected through histopathological examination of colonic biopsies. The nature of these microscopic changes is what differentiates collagenous from lymphocytic colitis, with the characteristic finding in collagenous colitis being depositions of collagen in the connective tissue between the colonic glands. Collagenous colitis, and microscopic colitis as a whole, is sometimes considered to be an inflammatory bowel disease (IBD) along with Crohn's disease and ulcerative colitis. However, little is known about the etiology of microscopic colitis, and so the degree of similarity to the inflammatory bowel diseases is uncertain.

<span class="mw-page-title-main">Balsalazide</span> Anti-inflammatory drug

Balsalazide is an anti-inflammatory drug used in the treatment of inflammatory bowel disease. It is sold under the brand names Giazo, Colazal in the US and Colazide in the UK. It is also sold in generic form in the US by several generic manufacturers.

<span class="mw-page-title-main">Giaconda (pharmaceutical company)</span>

Giaconda is an Australian biotechnology company headquartered in Sydney. The company was founded in 2004 to commercialise a number of drug combinations developed by Professor Thomas Borody, a Sydney-based gastroenterologist.

Management of ulcerative colitis involves first treating the acute symptoms of the disease, then maintaining remission. Ulcerative colitis is a form of colitis, a disease of the intestine, specifically the large intestine or colon, that includes characteristic ulcers, or open sores, in the colon. The main symptom of active disease is usually diarrhea mixed with blood, of gradual onset which often leads to anaemia. Ulcerative colitis is, however, a systemic disease that affects many parts of the body outside the intestine.

<span class="mw-page-title-main">Biological therapy for inflammatory bowel disease</span>

Biological therapy, the use of medications called biopharmaceuticals or biologics that are tailored to specifically target an immune or genetic mediator of disease, plays a major role in the treatment of inflammatory bowel disease. Even for diseases of unknown cause, molecules that are involved in the disease process have been identified, and can be targeted for biological therapy. Many of these molecules, which are mainly cytokines, are directly involved in the immune system. Biological therapy has found a niche in the management of cancer, autoimmune diseases, and diseases of unknown cause that result in symptoms due to immune related mechanisms.

<span class="mw-page-title-main">Pancolitis</span> Medical condition

Pancolitis, in its most general sense, refers to inflammation of the entire colon. This can be caused by a variety of things. Pancolitis or universal colitis is frequently used in a more specific fashion to denote a very severe form of ulcerative colitis. This form of ulcerative colitis is spread throughout the entire large intestine including the right colon, the left colon, the transverse colon, descending colon, and the rectum. A diagnosis can be made using a number of techniques but the most accurate method is direct visualization via a colonoscopy. Symptoms are similar to those of ulcerative colitis but more severe and affect the entire large intestine. Patients with ulcerative colitis generally exhibit symptoms including rectal bleeding as a result of ulcers, pain in the abdominal region, inflammation in varying degrees, and diarrhea. Pancolitis patients exhibit these symptoms and may also experience fatigue, fever, and night sweats. Due to the loss of function in the large intestine patients may lose large amounts of weight from being unable to procure nutrients from food. In other cases the blood loss from ulcers can result in anemia which can be treated with iron supplements. Additionally, due to the chronic nature of most cases of pancolitis, patients have a higher chance of developing colon cancer.

Vedolizumab, sold under the brand name Entyvio, is a monoclonal antibody medication developed by Millennium Pharmaceuticals, Inc. for the treatment of ulcerative colitis and Crohn's disease. It binds to integrin α4β7, blocking the α4β7 integrin results in gut-selective anti-inflammatory activity.

<span class="mw-page-title-main">Alicaforsen</span> Chemical compound

Alicaforsen is an antisense oligonucleotide therapeutic that targets the messenger RNA for the production of human ICAM-1 receptor and is being developed for the treatment of acute disease flares in moderate to severe Inflammatory Bowel Disease (IBD).

<span class="mw-page-title-main">Colonic ulcer</span> Medical condition

Colonic ulcer can occur at any age, in children however they are rare. Most common symptoms are abdominal pain and hematochezia.

<span class="mw-page-title-main">Segmental colitis associated with diverticulosis</span> Medical condition

Segmental colitis associated with diverticulosis (SCAD) is a condition characterized by localized inflammation in the colon, which spares the rectum and is associated with multiple sac-like protrusions or pouches in the wall of the colon (diverticulosis). Unlike diverticulitis, SCAD involves inflammation of the colon between diverticula, while sparing the diverticular orifices. SCAD may lead to abdominal pain, especially in the left lower quadrant, intermittent rectal bleeding and chronic diarrhea.

Shomron Ben-Horin is an Israeli physician, a co-founder & Chief Medical Officer of Evinature, and professor of medicine at the Tel-Aviv University.

References

  1. "Olsalazine (Dipentum) Use During Pregnancy". Drugs.com. 6 September 2019. Retrieved 9 October 2020.
  2. "Olsalazine--a further choice in ulcerative colitis". Drug and Therapeutics Bulletin. 28 (15): 57–8. July 1990. doi:10.1136/dtb.28.15.57. PMID   2131213. S2CID   7178709.
  3. Wadworth AN, Fitton A (April 1991). "Olsalazine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in inflammatory bowel disease". Drugs. 41 (4): 647–64. doi:10.2165/00003495-199141040-00009. PMID   1711964. S2CID   243654426.
  4. 1 2 "Olsalazine Sodium 250 mg Capsules - Summary of Product Characteristics (SmPC) - (emc)". www.medicines.org.uk. Retrieved 9 January 2021.
  5. "Giaconda gets European patent for drug". The Sydney Morning Herald. 28 December 2006. Retrieved 16 January 2021.