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Drugs used in Tx of GI diseases
Pharmacology of GI drugs
108
Pharmacology
Professional
10/10/2011

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Term
PPIs: MOA?
Definition
irreversible blockage of H+K+-ATPase pump in parietal cells
Term
what are the effects of PPIs?
Definition
long lasting reduction of stimulated and nocturnal acid secretion
Term
How do the half-lives of PPIs compare to DOA?
Definition
shorter than DOA
Term
PPIs- tox?
Definition
may reduce absorption of some drugs and increase that of others
Term
What are the effects of H2 receptor blockers like cimetidine?
Definition
reduction of nocturnal acid, but less effective against stimulated secretion
Term
Cimetidine has which special side effects?
Definition
weak antiandrogenic agent, potent CYP inhibitor
Term
What does sucralfate do? How many times/day is it given?
Definition
polymerizes at site of tissue damage and protects against further damage, very insoluble with no systemic effects, must be given 4xday
Term
What is the MOA of metoclopramide?
Definition
D2 receptor blocker, removes inhibition of Ach neurons in END
Term
What are the effects of metoclopramide?
Definition
increases gastric emptying and intestinal motility
Term
What is metoclopramide used for?
Definition
gastric paresis, and as an antiemetic
Term
metoclopramide: tox?
Definition
parkinsonian symptoms due to block of CNS D2 receptors
Term
Domperidone is like which other drug? Is has less effect on what system?
Definition
metoclopramide, CNS
Term
Which cholinomimetic drug is used for colonic pseudo-obstruction in hospitalized pts?
Definition
neostigmine
Term
Which antibiotic is useful in diabetic gastroparesis, but tolerance often develops?
Definition
macrolides- erythromycin
Term
How do magnesium hydroxide and other nonabsorbable salts and sugars act as laxatives?
Definition
osmotic agents increase water content of stool
Term
what are the effects of MgOH and other osmotic laxatives?
Definition
causes evacuation within 4-6h, sooner in large doses
Term
what are MgOH and other osmotic laxatives used for?
Definition
simple constipation, bowel prep
Term
MgOH - tox?
Definition
may be absorbed and cause toxicity in renal impairment
Term
What do methylcellulose, psyllium, etc do?
Definition
increase volume of colon (bulk-forming laxative) and stimulate evacuation
Term
How do senna and cascara work?
Definition
They are stimulants, may cause cramping
Term
Which laxatives are stool surfactants?
Definition
docusate and mineral oil - lubricate stool and ease passage
Term
How does Lubrprostone work as a laxative?
Definition
stimulates chloride secretion into intestine, increasing fluid content
Term
Which opioid receptor antagonists are used as laxatives?
Definition
alvimopan, methylnaltrexone, blocks intestinal m-opioid receptors but does not enter CNS
Term
What is Tegaserod?
Definition
5-HT4 agonist, activates enteric 5-HT4 receptors and increases intestinal motility
Term
Loperamide (immodium): MOA?
Definition
activates m-opioid receptors in ENS
Term
Loperamide- effects?
Definition
slows motility in gut with negligible CNS effects
Term
Clinical applications for loperamide?
Definition
nonspecific, noninfectious diarrhea
Term
loperamide- tox?
Definition
mild cramping but little or no CNS toxicity
Term
diphenoxylate (lomotil): similar to?
Definition
loperamide, but high doses can cause CNS opioid effects and toxicity
Term
colloidal bismuth compounds: subsalicylate and citrate salts available - OTC preps are popular and have some value in...
Definition
traveler's diarrhea, due to absorption of toxins
Term
What is kaolin + pectin?
Definition
adsorbent compounds available OTC, anti-diarrheal
Term
Alosetron: MOA?
Definition
5-HT3 antagonist of high potency and duration of binding
Term
Alosetron: effects?
Definition
reduces smooth muscle activity in gut
Term
What is alosetron used for?
Definition
severe diarrhea-predominant IBS in women
Term
alosetron: tox?
Definition
rare but serious constipation, ischemic colitis, infarction
Term
Why are anticholinergics used in IBS?
Definition
nonselective action on gut activity, usually associated with typical antimuscarinic toxicity
Term
What is the chloride channel activator used in IBS? For whom specifically is it used?
Definition
lubiprostone, useful in constipation-predominant IBS in women
Term
odansetron: MOA?
Definition
5-HT3 blockage in gut and CNS with shorter duration of binding than alosetron
Term
odansetron: effects?
Definition
extremely effective in preventing chemotherapy-induced and postop N/V
Term
What are first-line antiemetic agents in cancer chemotherapy, and also used for post-op emesis?
Definition
odansetron and other 5-HT3 blockers
Term
How is odansetron given? tox?
Definition
usually IV but orally active in prophylaxis, very low toxicity but can slow colonic transit
Term
Aprepitant: MOA?
Definition
NK1-receptor blocker in CNS
Term
What are the effects of aprepitant?
Definition
interferes with vomiting reflex, no effect on 5-HT, dopamine, or steroid recepts
Term
aprepitant - clinical applications?
Definition
effective in reducing both early and delayed emesis in cancer chemotherapy
Term
how is aprepitant given? What is the IV form? tox?
Definition
orally, fosaprepitant, fatigue, dizziness, diarrhea, CYP interactions
Term
Which drugs are useful in antiemetic IV cocktails through unknown mechanisms?
Definition
corticosteroids
Term
What is scopolamine? What is it used for?
Definition
antimuscarinic, effective in emesis due to motion sickness but not other types
Term
What kind of efficacy do antihistaminics have in for anti-emesis action?
Definition
moderate efficacy in motion sickness and chemotherapy-induced emesis
Term
How do phenothiazines act to help with emesis?
Definition
act through block of D2 and muscarinic recepts
Term
Which cannabinoid is available for use in chemotherapy-induced nausea and vomiting but is associated with CNS effects?
Definition
dronabinol
Term
What is the MOA of 5-aminosalicylates (mesalamine) and sulfasalazine for IBD treatment?
Definition
uncertain, may be inhibition of eicosanoid inflammatory mediators
Term
What are the effects of 5-aminosalicylates (mesalamine) and sulfasalazine for IBD treatment?
Definition
topical therapeutic action, systemic absorption may cause toxicity
Term
what are the clinical applications of 5-aminosalicylates (mesalamine) and sulfasalazine?
Definition
mild-mod Crohn's and UC
Term
5-aminosalicylates (mesalamine) and sulfasalazine for IBD treatment - toxicity?
Definition
sulfasalazine causes sulfonamide toxicity and may cause GI upset, myalgias, arthralgias, myelosuppression, other aminosalicylates are much less toxic
Term
Purine analogues and antimetabolites, eg 6-mercaptopurine, methotrexate: MOA?
Definition
uncertain, may promote apoptosis of immune cells, methotrexate blocks dihydrofolate reductase
Term
Purine analogues and antimetabolites, eg 6-mercaptopurine, methotrexate: effects?
Definition
general suppression of immune processes
Term
Purine analogues and antimetabolites, eg 6-mercaptopurine, methotrexate: clinical applications among GI disorders?
Definition
mod-severe Crohn's and UC
Term
Purine analogues and antimetabolites, eg 6-mercaptopurine, methotrexate: toxicity?
Definition
GI upset, mucositis, myelosuppression, purine analogues may cause hepatotoxicity, but rare with methotrexate at dose used
Term
Anti-TNF antibodies (infliximab, others): MOA?
Definition
bind TNF, prevent it from binding receptors
Term
Anti-TNF antibodies (infliximab, others): effects for GI disorders?
Definition
suppression of several aspects of immune function, especially Th1 lymphocytes
Term
Anti-TNF antibodies (infliximab, others): clinical applications among GI disorders?
Definition
infliximab: mod-severe Crohn's and UC, others approves in Crohn's
Term
Anti-TNF antibodies (infliximab, others): toxicity?
Definition
infusion rxns, reactivation of latent TB, increased risk of dangerous systemic fungal and bacterial infections
Term
Pancrelipase: MOA and effects?
Definition
replacement enzymes from animal pancreatic extracts, improves digestion of fat, protein and carbs
Term
Pancrelipase: applications? How often do you take it? tox?
Definition
pancreatic insufficiency, with every meal, may increase incidence of gout
Term
Pancreatin is similar to pancrelipase but...
Definition
has lower potency, is rarely used
Term
Ursodiol: MOA?
Definition
reduces cholesterol secretion into bile
Term
ursodiol: effects?
Definition
dissolves gall stones
Term
ursodiol: clinical applications?
Definition
gall stones in pts refusing or not eligible for Sx
Term
ursodiol: tox?
Definition
may cause diarrhea
Term
Octreotide: MOA?
Definition
somatostatin analogue, mechanism not certain
Term
octreotide: effects?
Definition
may alter portal blood flow and variceal pressures
Term
octreotide: clinical applications?
Definition
pts with bleeding varices or at high risk of repeat bleeding
Term
octreotide: tox?
Definition
reduced endocrine and exocrine pancreatic activity, other endocrine abnormalities, GI upset
Term
What effect do beta-blockers have for treatment of varices?
Definition
reduce CO and splanchnic vascular resistance
Term
Which H2 blockers cause less CNS and sexual disturbance than cimetidine?
Definition
ranitidine (zantac), famotidine (pepsid), nizatadine (axid)
Term
Which H2 blockers are only PO?
Definition
famotidine (pepsid), nizatidine
Term
Which H2 blockers have less P450 inhibition? no P450 inhibition?
Definition
ranitidine (zantac), famotidine (pepsid) and nizatidine (axid)
Term
Which H2 blockers have increased first pass metabolism?
Definition
ranitidine (zantac)
Term
Aluminum salts given for antacid effect will cause...
Definition
constipation
Term
Which antacids cause constipation?
Definition
aluminum salts, Ca carbonate
Term
Which antacids cause diarrhea?
Definition
magnesium salts
Term
Which antacids are contraindicated in renal failure?
Definition
magnesium salts
Term
which antacids are preferred pre-op due to lower risk of aspiration pneumonitis?
Definition
sodium citrate
Term
Metabolic alkalosis, hemorrhoids and fissures, and milk-alkali syndrome can be caused by which antacids?
Definition
Ca carbonate
Term
Sucralfate contains aluminum which can cause...
Definition
constipation
Term
Metoclopramide can cause HTN when coadministered with...
Definition
MAOIs
Term
Cisapride increases ___ and rate of ____
Definition
Ach, gastric emptying
Term
Omeprazole has what effect on P450? constipation or diarrhea? What kind of tumor is associated with it?
Definition
inhibition, constipation, carcinoid tumor
Term
Misoprostole is a ____ analogue, and causes ____
Definition
PGE, abortion
Term
Misoprostole increases...
Definition
bicarb and mucin
Term
Of the opioid anti-diarrheal drugs, which has no drug interactions?
Definition
loperamide (imodium)
Term
Of the opioid anti-diarrheal drugs, which overdose is treated with naloxone?
Definition
loperamide (imodium)
Term
Of the opioid anti-diarrheal drugs, which is dosed in drops?
Definition
opium tincture
Term
Of the opioid anti-diarrheal drugs, which is used in convulsive states?
Definition
paragoric
Term
Of the opioid anti-diarrheal drugs, which has a greater risk of hypotension with anesthetics or phenothiazine?
Definition
paragoric
Term
Of the opioid anti-diarrheal drugs, which is also available IM?
Definition
codeine
Term
Of the adsorbent anti-diarrheal drugs, which is used for traveler's diarrhea prophylaxis?
Definition
bismuth
Term
Of the adsorbent anti-diarrheal drugs, which is contraindicated in ASA sensitivity?
Definition
bismuth
Term
Of the adsorbent anti-diarrheal drugs, which increases the concentration of oral anticoagulants and hypoglycemics?
Definition
bismuth
Term
Of the adsorbent anti-diarrheal drugs, which decreases the effects of uricosuric drugs?
Definition
bismuth
Term
Of the adsorbent anti-diarrheal drugs, which decreases the absorption of many drugs?
Definition
kaopectate, cholestyramine
Term
Of the adsorbent anti-diarrheal drugs, which may increase K+ loss?
Definition
kaopectate
Term
Of the adsorbent anti-diarrheal drugs, which is given for diarrhea caused by C Diff or bile?
Definition
cholestyramine
Term
Of the laxatives, which may damage nerves?
Definition
senna, castor oil
Term
Of the laxatives, which are like psyllium?
Definition
methylcellulose, Ca polycarbophil
Term
Of the laxatives, which are stimulants and carthartics?
Definition
bisacodyl, phenolphthalein, danthron, senna, castor oil
Term
Of the laxatives, which is metabolized in the intestine to ricinoleate, a surfactant?
Definition
castor oil
Term
Of the laxatives, which improves penetration of water and fat into feces?
Definition
docusate
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