Lecture 6 - Chemistry of Drugs to treat GIT Inflammation Flashcards
what kind of drug is sulfasalazne
a prodrug
what is sulfasalazine broken down to?
Active 5-aminosalisilic acid (5-ASA) (mesalazine)
what is the site of action of sulfasalazine?
the colon
what does sulfasalazine possibly inhibit?
prostaglandin and leukotriene biosynthesis
what is the environment of the colon?
low in oxygen and pH between 6 and 7
What happens to sulfasalazine in the colon?
bacterial azo-reductases cleave the sulfasalazine azo bond
How is sulfasalazine administered?
as an oral coated tablet
what pH does sulfasalazine disintegrate at?
pH = 7
How else can sulfasalazine be administered?
by rectum in suppositories or enema
Why is sulfasalazine targeted to the colon?
there are very few microorganisms in the stomach that can break down the azo group to the active form in the stomach
How is 5-ASA absorbed?
via gaps in the epithelial cells
What is the benefit of olsalazine and balasalazide?
they are cleaved and there is no sulfa-pyridyl toxicity
