mesalamine rectal

Action and Spectrum

Actions and Spectrum 

Mesalamine reduces IBD symptoms to lower inflammation in the lining of the colon and rectum.

It inhibits the production of inflammatory mediators in the colon with cyclooxygenase and lipoxygenase pathways.

Drug Interaction

Adverse Reaction

Frequency defined  

1-10% 

Rash (1.2%) 

Dizziness (3%) 

Acne (1.2%) 

Rectal pain (1.8%) 

Colitis (1.2%) 

Fever (1.2%) 

Black Box Warning

None

Contraindication / Caution

Contraindication: 

• Intolerance to salicylates, mesalamine or any of the ingredients in the mesalamine rectal product. 

Caution:  

• Patients who have a history of renal disease or renal impairment should use with caution. 
• Use with caution in patients who have previously experienced sulfasalazine allergies since mesalamine cross-reactivity can happen. 
• In patients who have a history of liver illness, use with caution. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

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

Mesalamine inhibits the production of cytokines, prostaglandins, and leukotrienes, prostaglandin. These helps to reduce swelling and repair of inflammatory tissue in the colon and rectum.

Pharmacodynamics:

Mesalamine suppresses nuclear factor kappa B and acts as a free radical scavenger to reduce oxidative stress.

Rectal mesalamine targets inflamed mucosa in rectum and colon, hence administered for high concentrations.

Pharmacokinetic:

Absorption:

The systemic absorption for rectal suppository is 15 to 38%.

Metabolism:

It is metabolized in colon wall and liver.

Excretion and elimination:

Half-life:

Rectal: 1.5 to 5 hours

Adminstartion

It is administered rectally in the suppository form.

Patient Information Leaflet

Generic Name: mesalamine rectal

Why do we use mesalamine rectal?

Mesalamine rectal is used in treatment of ulcerative colitis which causes inflammation of the rectum and lower colon.

Mesalamine rectal suppositories are used for treating ulcerative proctitis.