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GI 2
Pharm
87
Medical
Kindergarten
04/28/2010

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Term
How much of the 9 L (2L from diet 7 from secretions) that is presented to the intestines is reabsorbed?
Definition
99%
Term
What things can casue diarrhea
Definition
increased osmotic load, excessive secretion of electrolytes and water, exudation of protein and fluid from mucosa, altered intestinal motility... basically, a failure to reabsorb
Term
What are the 3 classifications of intraluminal agents that are anti-diarrheal?
Definition
Hydroscopic agents, Bile acid resins, and Bismuth Subsalicylate
Term
What are the 3 Hydroscopic agents?
Definition
psyllium, kallin, and pectin
Term
What is the MOA of Hydroscopic agents?
Definition
absorb water and increase stool bulk, may also bind bacterial toxins
Term
What are the 2 Bile acid resins used as anti-diarrheals?
Definition
Cholestyramine and Colestipol
Term
What is the MOA of Bile acid resins used as anti-diarrheals?
Definition
They bind bile acids and are useful in bile salt-induced diarrhea and may also bind bacterial toxins
Term
What is a drawback of Bile acid resin use for anti-diarrhea treatment?
Definition
sequester thyroxin, digoxin and vitamins. decreased bioavailability of those drugs
Term
What drug is found in Peptobismol and is used as an anti-diarrheal?
Definition
Bismuth Subsalicylate
Term
WHat is the MOA of Bismuth Subsalicylate?
Definition
forms bismuth oxychloride which is not absorbed and salicylic acid that is absorbed
Term
What is the action of Bismuth
Definition
sepcifically, from Bismuth Subsalicylate?,it is anti-secretroy, anti-inflammatroy, and anti-microbial
Term
What is the action of Salicylic acid
Definition
from Bismuth Subsalicylate, specifically?,it is anti-inflammatory
Term
What is a side effect of Bismuth Subsalicylate and what is it due to?
Definition
It can turn the tongue and stool black. It is due to Bismuth Sulfide.
Term
What are the two opioids used as Anti-diarrheals?
Definition
Loperamide and Diphenoxylate
Term
What is the MOA of opioids as antidiarrheals?
Definition
activate intestinal mu receptors, causing tonic contraction. They also activate mu and delta receptors for absorption.
Term
What is the potency of Loperamide and Diphenoxylate as antidiarrheals
Definition
as compared to Morphine?,more potent than morphine for anti-diarrheal activity.
Term
What is the big difference in the two opioids that are used as anti-diarrheals?
Definition
Their ability to cross the BBB
Term
What are loperamide's actions?
Definition
penetrates the CNS poorly, increases rectal sphincter tone, disrupts peristalsis
Term
What are the actions of Diphenoxylate?
Definition
can penetrate the CNS causing respiratory depression
Term
What do preparations of Diphenoxylate include?
Definition
atropine, to reduce secretion and motility and to discourage abuse
Term
WHat is the main side effect of Opioids used as anti-diarrheals?
Definition
Constipation
Term
What is the MOA of Clonidine as an anti-diarrheal?
Definition
alpha-2 agonist; it activates receptors that stimulate absorption, inhibit secretion, and increase intestinal transit time
Term
What is the main use of Clonidine as an anti-diarrheal?
Definition
USed to treat diabetics with chronic diarrhea due to autonomic neuropathy
Term
What is the MOA of Octretotide as an anti-diarrheal?
Definition
it is an inhibitory analog of Somatostatin. It inhibits secretion, decreases contractility
Term
What is the potency and duration of action of Octeotride compared to Somatostatin?
Definition
much more potent and longer half life
Term
How is Octreotide administered?
Definition
SubQ or IM
Term
What are the indications for Octreotide use for diarrhea?
Definition
Carcinoid Syndrome, VIPoma, AIDS, Diabetes
Term
What is the side effect of Octreotide?
Definition
gall stone formation
Term
What are the 5 classifications of laxative mechanism?
Definition
Bulk laxatives, Lubricating agents, Stimulant laxatives, Osmotic agents, Neuromuscular agents
Term
WHat are the 2 Bulk laxatives?
Definition
psyllium and methylcellulose
Term
What are some drawbacks of Bulk laxatives?
Definition
can undergo bacterial degradation in the colon and cause bloating and flatulence, unpleaseant to swallow, can bing drugs such as digoxin and thyroid hormone
Term
What is the speed of action of bulk laxatives?
Definition
slow acting
Term
What are the effects of bulk laxatives?
Definition
increase stool bulk and shorten intestinal transit time
Term
What is a lubricating agent used as a laxative which softens stool over 2-3 days?
Definition
Mineral oil
Term
What does Mineral oil interfere with?
Definition
it is indigestable, so it interferes with aborption of fat soluble things
Term
What are adverse effects of Mineral oil?
Definition
interruption of fat soluble substance absorption, anal sphincter oil leakage and oil aspiration in childrena nd elderly
Term
What are the 4 stimulant laxatives?
Definition
docusate, bisacodyl, senna, and castor oil
Term
What is the MOA of Docusate?
Definition
it is a SURFACE-acting agent that softens the stool, but also increases electrolyte and water secretion into the intestinal lumen
Term
What do all stimulant laxatives work to do?
Definition
they cause a PG-mediatedincrease in cAMP but also inhibit Na/K ATPase, leading to electrolyte and water secretion and also cause low grade inflammation
Term
What do stimulant laxatives induce in the small and large bowel?
Definition
low grade inflammation
Term
WHen is Docusate used as a stimulant laxative?
Definition
following colorectal surgery and post-MI to reduce strain
Term
How is Bisacodyl administered and how does it act?
Definition
enteric-coated capsules; works just like Docusate by causing increased electrolyte and water secretion by a PG-mediated increase in cAMP and inhibition of Na/K ATPase
Term
What are the anthroquinones that are used as stimulant laxatives?
Definition
Senna*, aloe, rhubarb
Term
What is the onset of action of Anthroquinones and what do they produce?
Definition
delayed; produce giant migrating colonic contractions
Term
How does Castor oil work as a stimulant laxative?
Definition
causes low grade inflammation in the small bowel, causing water and electrolyte secretion.
Term
What are the Osmotic agents taht are used as laxatives?
Definition
Saline laxatives, poorly absorbed sugars, PEG, lubiprostone
Term
What are the saline laxatives?
Definition
Magnesium Hydroxide, Sodium Phosphate, Magnesium Citrate
Term
WHen is Magnesium Hydroxide used?
Definition
for acute and chronic constipation
Term
When is Magnesium citrate used?
Definition
as a cathartic
Term
What are the poorly absrobed sugars used as laxatives?
Definition
lactulose, sorbitol, mannitol
Term
what is the MOA of poorly metabolized sugars (lactulose
Definition
sorbitol, mannitol) as laxatives?,They are hydrolyzed by intestinal bacteria, acidified, and create osmotic drag
Term
What laxatives are used before bowel procedures?
Definition
Polyethylene glycol-electrolyte containing solutions
Term
What is the MOA of PEG containt solutions?
Definition
They are poorly absorbed and cause water retention in the colon
Term
What is a fatty acid metabolite of PGE1 that activates Cl- channels in the GI epithelium?
Definition
Lubiprostone
Term
What is the effect of Lubiprostone activation of Cl- channels in the GI epithelium?
Definition
stimulates intestinal fluid secretion and decreases intestinal transit time
Term
What is Lubiprostone used for?
Definition
chronic idiopathic constipation in adults and constipation a/w IBS
Term
What are the side effects of Lubiprostone?
Definition
nausea and diarrhea
Term
What are examples of Neuromuscular agents that are used as laxatives?
Definition
5HT4 agonists, Misoprostol (PG), cholinergics (bethanechol-direct, Neostigmine-indirect), opiate antagonists
Term
What is a selective mu receptor antagonist that is used for opioid induced constipation
Definition
Methylnaltrexone
Term
When is Methylnaltrexone used?
Definition
In patients with advanced illness that are receiving opioid pain meds, which induce constipation.
Term
WHy is Methylnltrexone used in patients on opioid analgesics?
Definition
Because it blocks GI mu receptors without affecting analgesic effects of other mu receptors
Term
What are the 2 divisions of Inflammatory Bowel DISEASE?
Definition
Ulcerative Colitis and Chron's
Term
What 6 calsses of drugs are used for Inflammatory Bowel Dz treatment?
Definition
1. Sulfasalazine
Term
What are the 2 components of Sulfasalazine?
Definition
Mesalamine and Sulfapyridine
Term
What is the MOA of Mesalamine?
Definition
It inhibits COX and Lipoxygenase, reducing LTB4 and 5_HETE levels
Term
Which component of Sulfasalazine is responsible for most of the side effects
Definition
the Mesalamine or Sulfapyridine?
Term
What are the uses of Sulfasalazine?
Definition
acute and maintenance therapy of Ulcerative Colitis
Term
What are the side effects of Sulfasalazine
Definition
which are mediated by the Sulfapyridine component?,Fever, malaise, headache, skin rash, bone marrow suppression.
Term
When is Mesalamine used?
Definition
It is more effective for Tx of Chron's and it is used in acute and maintenance therapy for Ulcerative Colitis
Term
What are the side effects of Mesalamine like compared to Sulfasalazine and what are they?
Definition
Muche less. They include headache, rash, and diarrhea
Term
Why are Glucocorticoids indicated in Treatment of Inflammatory Bowel Disease?
Definition
for their anti-inflammatory actions
Term
What are the systemic side effects of oral Prednisone?
Definition
HTN, Hypoglycemia, cataracts, mood change
Term
What are the 4 Immunomodulators used for Treatment of Inflammatory Bowel disease?
Definition
Mercaptopurine, Azathioprine, Methotrexate, cyclosporine
Term
How do Meracptopurine and Azathioprine work as immunomodulators?
Definition
Mercaptopurine suppresses Lymphocyte proliferation; Azathioprine is converted to Mercaptopurine
Term
How does Methotrexate work as an immunomodulator?
Definition
It is a DHFR inhibitor with anti-inflammatory and immunosuppressive activity
Term
How does Cylcosporine work as an immunomodulator?
Definition
It inhibits T cell activation
Term
What are the biological agents used in the treatment of Inflammatory Bowel Disease?
Definition
Infliximab, Adalimumab, Certolizumab, Natalizumab
Term
What is the MOA of Infliximab?
Definition
monoclonal Ab to TNF-alpha
Term
What is the MOA of Adalimumab?
Definition
humanized Ab to TNF-alpha
Term
What
Definition
besides Inflammatory Bowel Dz, is Adalimumab used to treat?,R.A.
Term
What is the MOA of Certolizumab?
Definition
It is a Fab fragment to TNF alpha
Term
What is the MOA of Natalizumab?
Definition
It is a monoclonal Ab to alpha4 integrins, which are key in leukocyte trafficking and cell-cell communication during inflammation
Term
Which 2 antibiotics are used in the Treatment of Inflammatory Bowel Disease?
Definition
Metronidazole and Ciprofloxacin
Term
What is a 5HT4 agonist used for the treatment of constipation a/w Inflammatory Bowel Dz?
Definition
Tegaserod
Term
What is a 5HT3 antagonist used for treatment of diarrhea associated with Inflammatory Bowel Dz?
Definition
Alosetron
Term
What are the anti-spasmodics used for bloating a/w Inflammatory Bowel Dz? (a general class of drugs)
Definition
anti-cholinergics
Term
What 3 classes of drugs are used for the treatment of abdominal pain a/w Inflammatory Bowel Dz?
Definition
anti-cholinergics, TCA's, SSRI's
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