olsalazine

Action and Spectrum

Actions and Spectrum 

olsalazine works by inhibiting the production of prostaglandins and leukotrienes, suppressing the production of inflammatory cytokines and decreasing inflammation. 

olsalazine’s range of action is restricted to the colon and rectum because it is not absorbed into the bloodstream and has no systemic consequences. 

Drug Interaction

Adverse Reaction

Frequency not defined  

1-10% 

Arthralgia (4%) 

Anorexia (1.3%) 

Dyspepsia (4%) 

Depression (1.5%) 

Dizziness (1%) 

Bloating (1.5%) 

Joint pain (4%) 

Upper respiratory infection (1.5%) 

Nausea/vomiting (6%) 

Rash/itching (3.6%) 

Fatigue (1.8%) 

Headache (5%) 

>10% 

Abdominal pain (11%) 

Diarrhea (17%) 

Post marketing reports 

Skin and subcutaneous tissue disorders: Angioneurotic edema 

Thoracic, respiratory and mediastinal disorders: Interstitial lung disease, pleurisy/pleuritis, Dyspnea 

Black Box Warning

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• allergy or hypersensitivity to olsalazine or any of its ingredients 

Caution: 

• severe liver condition 
• serious renal condition 
• bleeding issues 
• known sensitivity or allergy to drugs 
• breastfeeding or pregnant 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: C 

Lactation: Excretion into human milk is unknown  

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology 

Two molecules of 5-aminosalicylic acid (5-ASA) are found in the drug olsalazine, which is joined by an azo bond. olsalazine stays in the colon after consumption and is broken down by bacterial enzymes to release the active component, 5-ASA. 

Pharmacodynamics 

olsalazine’s pharmacodynamics are mostly based on the activity of 5-aminosalicylic acid (5-ASA), which is its active component. 

5-ASA is an anti-inflammatory drug that reduces inflammation locally in the colon. It is believed to function by preventing the production of leukotrienes and prostaglandins, chemicals involved in the inflammatory process. The generation of inflammatory cytokines, which can aid in the onset of inflammatory bowel disease (IBD), is also suppressed by 5-ASA. 

Pharmacokinetics 

Absorption   

olsalazine remains in the colon where it is broken down by bacterial enzymes to produce the active component, 5-aminosalicylic acid (5-ASA), as it is not absorbed from the gastrointestinal system. olsalazine has less systemic effects and a lower risk of negative effects because it is not absorbed. 

Distribution 

olsalazine and 5-ASA, the drug’s active component, do not significantly bind to plasma proteins and do not build up in the body. olsalazine does not disperse widely throughout the body since it is not absorbed. 

Metabolism 

In the colon, bacterial enzymes degrade olsalazine to release 5-ASA. 5-ASA is partially metabolized in the liver and eliminated through the urine. 

Elimination and excretion 

olsalazine and 5-ASA are mostly eliminated in the urine. 5-ASA has an elimination half-life of two to three hours. 

Adminstartion

Administration:  

olsalazine is a medication that can be taken orally as a capsule, usually two to three times per day. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: olsalazine 

Why do we use olsalazine? 

olsalazine is a drug mostly used to treat mild to moderate ulcerative colitis, a form of inflammatory bowel disease that damages the lining of the colon and rectum.