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