PBL 1 Flashcards
what are the indications for loperamide?
control and symptomatic relief of acute nonspecific diarrhoea and chronic diarrhoea associated with IBD
what is loparamides moa?
its a non-selective Ca2+ channel blocker and binds to opioid mu-receptors in the myenteric plexus in the large intestine
it decreases myenteric plexus activity which decreases motility, this increases the time substances stay in the intestine and so increases water absorption = decreases colonic mass moveemnts
what are the 2 main classifications for antispasmodics?
antimuscarinics (anticholinergics) and smooth muscle relaxants
what do antimuscarinics do?
reduce intestinal motility
what are antimuscarinics used for?
gastrointestinal smooth muscle spasm
what are examples of antimuscarinics?
atropine sulface
diccloverine hydrochloride
propantheline bromide
hyoscine butylbromide
what are smooth muscle relaxants used for?
relieveing abdominal pain or spasm in IBS
what are examples of smooth muscle relaxants?
Alverine citrate, mebeverine hydrochloride, and peppermint oil
what is azathioprine used for?
IBD as its an immunosuppressive drug
what is azathioprines moa?
inhibits purine synthesis so less DNA and RNA are formed = less synthesis of WBCs = immunosuppression
what are examples of aminosalicylates?
5-aminosalicylate and sulfasalazine
what is sulfasalazines moa?
inhibits folic acid and splits into its metabolites 5-ASA and sulfapyridine
why do we often give 5-ASA alone rather than as a product of sulfasalazine breakdown?
as sulfapyridine (also a breakdown product of sulfasalazine) has side effects
why can 5-ASA have topical effects on the colonic epithelium? (why not digested before)
its poorly absorbed by the intestine and systemic circulation
outline 5-ASAs moa?
its metabolised in the colon into N-acetyl-5-ASA by N-acetyl-transferase-1. It then binds a nulcear hormone receptor which induces the translocation into the cell nucleus with the reception. here it can control transcription and modulate the expression of pro-inflammatory cytokines and prostaglandins