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35 Cards in this Set

  • Front
  • Back
What is Loperamide used for in IBS?
NS tx for pts with predominant diarrhea
What drug class is Amitryptaline in?
TCA
What drug class is Desipramine in?
TCA
How are TCAs (Amitryptaline and Desipramine) used in IBS?
used at doses lower than to tx diarrhea IBS
Name 3 SSRIs talked about in this lecture
Paroxetine, Fluoxetine, Sertaline
What are SSRIs (Paroxetine, Fluoxetine, Sertaline) used for in IBS?
May be beneficial in the NS tx of constipation IBS
MOA of Alosteron
5HT3 antagonist (used to tx diarrhea IBS)
MOA of Tegaserod
selective 5HT4 agonist (used to tx constipation IBS); stimulate 5HT4 receptor-->CGRP release from myenteric and submucosal plexuses-->peristalsis-->proximal bowel contraction (via ACh and SP) and distal bowel relaxation (NO and VIP)
What sets apart Alosteron from the other "sterons" used as antiemetics?
Alosteron has a higher affinity and dissociates more slowly from the 5HT3 receptor (LONGER DOA)
TU for Alosteron
Women with SEVERE diarrhea IBS who have not responded to other therapies
SE of Alosteron
Constipation in up to 30%; ischemic colitis; SE may be > with concomitant use of CYP1A2 inhibitors (i.e. fluvoxamine-SSRI)
Besides being a 5HT4 agonist, how else does Tegaserod tx constipation IBS?
activates cAMP dependent Cl- secretion
What pts should you use caution in prescribing Tegaserod?
those with hepatic or renal impairment (met in liver and excreted in urine)
When should pts take Tegaserod and why?
Before meals as it has a low bioavailability and food decreases this further
TU of Tegaserod in GI?
Constipation IBS
SE of Tegaserod
Voluntarily removed from the market due to cardio effects (prolongation of the QT interval)
What drug class is Balsalazide in?
Aminosalicylates/Anti-inflammatory
What drug class is Mesalamine in?
Aminosalicylates/Anti-inflammatory
What drug class is Olsalazine in?
Aminosalicylates/Anti-inflammatory
What drug class is Sulfasalazine in?
Aminosalicylates/Anti-inflammatory
Why do Balasalazide, Osalazine and Sulfasalazine have more topical effects than Mesalamine?
feature some moiety linked to 5-ASA which limits absorption until the bacteria in the colon break down the compounds, releasing 5-ASA
MOA of Aminosalicylates
Block PG synthesis by inhibiting COX
Drugs of choice for 1st line tx of mild-moderately active ulcerative colitis
Aminosalicylates (Mesalamine, Balasalazide, Osalazine and Sulfasalazine); suppositories or enemeas are effective
Which Aminosalicylate has a high incidence of SE (N/V, headache, arthralgias, BM suppression and malasie)
Sulfasalazine (HS rxns also occur)
Prednisone and Prednisolone are used in the tx of what? (in regards to GI)
moderate to severe active IBD
Which corticosteriod results in a local (GI) effect rather than systemic like the others?
Budesonide (subject to extensive, rapid 1st pass metabolism)
TU of Budesonide
Milde to moderate Crohn's disease involving the ileum and proximal colon
TU of antimetabolites (Azathioprine, 6-Mercaptopurine, Methotrexate)
induction and maintenance of remission of ulcerative colitis and Crohn's
Name the anti-TNF alpha antibodies used to tx IBD
Infliximab, Adalimumab, Certolizumab
Anti-TNF antibodies can lead to symptomatic improvement and remission in pts with what?
moderately severe Crohn's
Humanized anti-TNF?
Adalimumab (Infliximab and Certolizumab are chimeric)
Name 2 anti-TNFs that bind to both soluble and receptor bound TNFalpha?
Infliximab and Adalmumab (also, Fc promotes complement activation and Ab mediated cellular cytotoxicity of inflammatory cells)
Recombinant Ab consisting of a Fab component conjugated to PEG (NO Fc component, thus NO complement activation)
Certolizumab
SE of anti-TNFaphas
Infection, acute, adverse infusion rxns (Infliximab in particular), delayed infusion rxns, hepatic rxns, > risk for lymphoma
How may you reduce infusion rxns with anti-TNFalphas?
prophylactic administration of acetaminopehn, diphenydramine or corticosteroids