GI Part II Flashcards
Goals of mild constipation IBS treatment?
Increase dietary fiber and fluid intake
Goals of moderate constipation IBS treatment?
Add bulk forming laxatives with or without antispasmodics
Goals of severe constipation IBS treatment?
Add chloride channel activator
Goals of mild diarrhea IBS treatment?
- Dietary restriction
- Avoid contributing meds
Goals of moderate diarrhea IBS treatment?
-Add loperamide or other antispasmodics
Goals of severe diarrhea IBS treatment?
Add 5HT3 antagonists
IBS diarrhea drug choices
- Loperamide
- Anticholinergics
- Serotonin receptor blockers
IBS constipation drug choices
- Fiber supplements
- Osmotic laxatives
- Cl Channel Activators
- Guanylate Agonist
Describe antispasmodics
- Anticholinergic (anti-SLUD)
- Used for diarrhea
- Side effects are dry mouth, blurred vision, urinary retention, constipation
- Dicyclomine
What are TCAs and what type of IBS are they used to treat?
- Tricyclic Antidepressants
- Anticholinergic action
- Decreases GI secretion and motility
- Used for diarrhea
- May help chronic abdominal pain
- Amitriptyline, desipramine
What are 5HT3 receptor blockers and what type of IBS are they used to treat?
- Serotonin receptor blockers
- Mediate visceral pain
- Inhibits colonic motility
- Used for diarrhea
- Alosetron
What is Alosetron and how is it used?
- Selective 5HT3 blocker
- Used for severe diarrhea IBS in women (efficacy in men not established)
Side effects of Alosetron?
- Constipation (can be severe)
- Ischemic colitis (fatalities reported, black box warning)
Describe bulk forming laxatives
- Anti constipation
- Form bulky emollient gel that distends colon and promotes peristalsis
Describe osmotic laxatives
- Anti constipation
- Nonabsorbable compounds that result in increased stool liquidity (due to obligate increase in fecal fluid)
What are chloride channel activators?
- Approved for constipation IBS in women (efficacy in men not shown)
- Lubiprostone/Amitiza
What is Lubiprostone?
- Chloride channel activator
- For constipation IBS in women
- Works on small intestine
- Enhances Cl-rich secretions and intestinal motility
Contraindications of lubiprostone? Adverse effects?
- Avoid in women of CBP (preg cat C)
- Nausea, diarrhea, HA
What is linaclotide?
- Guanylate agonist
- Used for constipation
- Causes rise of cGMP leading to rise of Cl and bicarb into intestinal lumen
- Fluid increases, transit time decreases
Side effects of linaclotide?
- Diarrhea
- Flatulence
- GI upset
What are serotonin 5HT4 receptor blockers?
- Results in release of NTs promoting peristaltic reflex
- Proximal bowel contraction and distal bowel relaxation
- For constipation
- No agent available in US
Drug classes for IBD treatment
- Aminosalicylates
- Glucocorticoids
- Purine analogs
- MTX
- Anti-TNF
- Anti-integrins
Drugs for mild IBD
- 5-aminosalicylates
- Abx
- Topical corticosteroids
- Budesonide
Drugs for moderate IBD
- Azathioprine/6-mercaptopurine
- MTX
- Oral corticosteroids
- TNF blockers
Drugs for severe IBD
- IV corticosteroids
- TNF blockers
- Cyclosporine
- Natalizumab
- Surgery
What is the active compound of all aminosalicylates?
5-ASA
MOA of aminosalicylates?
Unclear
- May affect inflamm mediators
- May interfere w/cytokine production
- May inhibit immune cells
How do aminosalicylates work in IBD treatment?
- Topically on affected areas of GI mucosa
- So must get to affected site
- Pure oral 5-ASA is more than 80% absorbed which means little left over to go to needed area
- Formulations are made to avoid so much absorption
What are the different formulations of aminosalicylates?
- Azo compounds
- Mesalamine compounds
What are the azo aminosalicylate drugs?
- Sulfasalazine
- Olsalzine
- Balsalazide
What are the mesalamine aminosalicylate drugs?
- Pentasa
- Asacol
- Lialda
How do azo compounds work?
- N=N azo bond reduces absorption after oral absorption
- At ileum and colon, bacteria cleave the molecules and release active 5-ASA