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97 Cards in this Set
- Front
- Back
In which "GI class" of drugs is Cisapride?
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Prokinetics (> GI motility)
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In which "GI class" of drugs is Domeperidone?
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Prokinetics (> GI motility)
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In which "GI class" of drugs are the macrolide antibiotics (Erthromycin)?
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Prokinetics (> GI motility)
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In which "GI class" of drugs is Metoclopramide?
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Prokinetics (> GI motility)
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In which "GI class" of drugs is Diphenoxylate?
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Antidiarrheals (Opiates)
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In which "GI class" of drugs is Loperamide?
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Antidiarrheals (Opiates)
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In which "GI class" of drugs is Cholestyramine?
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Antidiarrheals (Bile Acid Binding)
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In which "GI class" of drugs is Colestipol?
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Antidiarrheal (Bile acid binding resins)
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In which "GI class" of drugs are Kaolin/Pectin?
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Antidiarrheal (Absorbants)
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In which "GI class" of drugs are Bismuth subsalicylate and Octerotide?
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Antidiarrheal
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In which "GI class" of drugs is Docusate?
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Stool Softner
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In which "GI class" of drugs is Mineral Oil?
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Stool Softner
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In which "GI class" of drugs is Psyllium?
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Bulk Lax
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In which "GI class" of drugs are Anthraquinone derivatives?
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Stimulant cathartics
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In which "GI class" of drugs is Cascara sagrada?
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Stimulant cathartics
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In which "GI class" of drugs is Danthron?
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Stimulant cathartics
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In which "GI class" of drugs is Senna?
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Stimulant cathartics
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In which "GI class" of drugs is Bisacodyl?
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Stimulant Cathartics
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In which "GI class" of drugs is castor oil?
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Stimulant Cathartics
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In which "GI class" of drugs is Lactulose?
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Osmotic cathartic
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In which "GI class" of drugs is Mg Hydroxide?
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Osmotic cathartic
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In which "GI class" of drugs is Na Phosphate?
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Osmotic cathartic
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In which "GI class" of drugs is Polyetheylene glycol solution?
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Osmotic cathartics
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In which "GI class" of drugs is Lubiprostone?
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Misc Lax & Cathartics
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In which "GI class" of drugs is Alvimopan?
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Opiod receptor antagonist: Misc Lax & Cathartics
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In which "GI class" of drugs is Methylnaltrexone?
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Opiod receptor antagonist: Misc Lax & Cathartics
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< motility does what to water absorption?
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increases water absorption
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What secretes ACh in regards to the GI system?
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Interneurons of the submucosal and myenteric plexi as well as pre and post gang of parasympathetics
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ACh does what in regards to the GI system? (General)
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> both motility and secretion
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What does Somatostatin do to intestinal and pancreatic secretions? To intestinal motility?
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decreases all of them; also inhibits gallbladder contraction
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The 4 big NTs that regulate motility and water absorption of the lower GI tract
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ACh, Serotonin (5HT), Dopamine and Enkephalins
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_____ interneurons in the myenteric plexus help to regulate the peristaltic reflex
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Cholinergic
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Class of Atropine
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ACh antagonist
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ACh will ____ motility and _____ water excretion
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Increase motility and Increase water excretion (decreases absorption)
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5HT1 will _____ water absorption
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Increase (by increasing NANC-mediated inhibition of water excretion)
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5HT3 will _____ distal relaxation
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increase by exciting NANC neurons
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5HT4 will ____ proximal contraction
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increase
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Dopamine (D2) will ____ ACh induced motility
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Decrease; thus < motility
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u Enkephalins stimulates what? (in regard to water)
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Stimulates 5HT1 increase in water absorption
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k and u Enkephalins ____ ACh induced motility
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INHIBIT
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The "SETRONs" are what class of drugs? What effect will do they have on the GI system?
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5HT3 Antagonistis; inhibit peristalsis, > contraction by decrease motility
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What class of drugs (agonist/antagonists) are Cisapride and Tegaserod and what effect do they have on the GI system?
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5HT4 Agonist; will > motility
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Name 2 D2 antagonists and their effects on the GI system
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Metoclopramide and Domperidone; will > motility
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Name 2 u enkephalin agonists and their effects on the GI system
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Diphenoxylate and Loperamide; < motility and secretion and > water absorption
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Name 2 k and u antagonists?
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> motility and > secretion
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One of the major roles for serotonin in the gut is thought to be regulation of the ________ reflex
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Peristaltic (consists of both a proximal contraction and distal relaxation)
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Bottom line: 5HT4 agonists ___ GI motility
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Increase GI motility (decrease transit time)
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Bottom line: 5HT3 antagonists ____contractility but _____ coordination
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Increase contractility but decrease coordination (increase transit time)
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What differentiates prokinetics from laxatives and cathartics?
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Lax and cathartics tend to act more indirectly, and to influence only the LI
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General MOA of Prokinetics
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> motility throughout entire GI tract; thought to be through actions on the enteric nervous system; > LES pressure
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Which Choolinomimetic has severe SE?
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Cisapride may cause fatal arrhythmias
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MOA of Metoclopramide and Domperidone
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D2 receptor antagonists; cause inhibition of dopamine inhibition of ACh induced contraction
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Between Metoclopramide and Domperidone, which has CNS effects?
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Metoclopramide has CNS effects and can be used as an antiemetic (Domperidone does not cros the BBB)
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MOA of Cisapride
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5HT4 agonist; partial 5HT3 antagonist
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MOA of Macrolide antibiotics (Erythromycin) in regards to GI
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stimulate motilin receptors -->initiation of migrating motor complex (at subclinical doses for antibiotic actions, still may cause resistance, however!)
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Therapeutic uses (although controversial) of Marcolides in regards to GI
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To tx impaired gastric emptying (vagotomy) and diabetic gastroparesis; GERD too although not as much since PPIs are around
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SE of dystonia, parkinsonism and Tardive dyskinesia if pts are given high doses; increased prolactin release (impotence, galactorrhea, menstrual disorders)
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Metoclopramide (prokinetic)
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In what sort of pts should antidiarrheals NOT be used
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those with bloody diarrhea, high fever or systemic toxicity
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Most effective agents to tx treatable forms of diarrhea
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Opiates (Diphenoxylate and Loperamide)
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How do Diphenoxylate and loperamide increase phasic colonic segmenting activity (motility)?
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Activating k and u receptors which inhibit cholinergic neurons and serotonergic neurons that regulate propulsion (Increased transit time!)
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How do Dipehnoxylate and Loperamide inhibit water excretion?
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Activation of serotinergic neurons (u) which stimulate 5HT1or2 receptors on enteric neurons that inhibit water excretion
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Between the Opiates Loperamide and Diphenoxylate, which one does NOT cross the BBB?
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Loperamide does not (available OTC)
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SE of the Opiates (Diphenoxylate and Loperamide)
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Toxic megacolon in given to pts with severe ulcerative colitis (at high doses, a physical dependence on Diphenoxylate may occur)
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MOA of Cholestyramine and Colestipol
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Bile acid binding resins
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Drugs used to tx diarrhea associated with malabsorption of bile salts (colonic secretory diarrhea); Crohn's disease or surgical resection
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Cholestyramine, Colestipol
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SE of Cholestyramine, Colestipol
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Bloatal, flatulence, imparied intestinal absorption of concurrently administered drugs and fat-soluble vitamins
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@ high doses, Somatostatin will ____ motility
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inhibit
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Synthetic analogue of Somatostatin
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Octerotide (inhibits gastric motility)
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Therapeutic uses of Octerotide
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Diarrhea due to vagotomy, dumping syndrome, short bowel, AIDS, tx effects of carcinoid tumors and VIPomas
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Gallstones in 50% of pts, Impaired pancreatic secretion (leading to fat soluble vitamin def and steatorrhea), hyper/hypoglycemia, hypothyroidism, bradycardia
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Octerotide
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MOA of Bismuth Subsalicylate in the LI
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inhibits PG and Cl- secretion in the LI (stimulates PG, mucous and Bicarb secretion in the stomach)
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Possible tx of Traveller's Diarrhea
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Opiates (most effective) and Bismuth Subsalicylate
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SE of Bismuth Subsalicylate
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Black stool and tongue; possible salicylate tox (tinnitus)
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MOA pectin
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indigestible carb (Absorbant)
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MOA of Kaolin
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naturally occurring Mg Al silicate (Absorbant)
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SE of absorbants (Kaolin and Pectin)
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May bind other medications
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Which will have a strong effect/short latency: lax or cathartics?
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Cathartics (Lax will have mild effect but long latency)
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Slowest of the lax and cathartics
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Stool softeners and bulk forming lax
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Acts as a surfactant and softens the stool by allowing mixing of aqueous and fatty substances
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Docusate
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Lubricates feces-->decreased water absorption from stool
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Mineral Oil
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SE of Mineral Oil
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Severe lipid pneumonitis is aspirated, < absorption of fat soluble vitamins
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Name the Bulk Lax
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Dietary fiber, Methylcellulose, Psyllium
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MOA of Bulk Lax
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> mass of stool-->distenstion-->enteric reflexes--> increase GI motility
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Name the fast acting Contact cathartics
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Anthraquinone derivatives (Senna, Dantrhon, Cascara sagrada), Bisacodyl and Castor Oil
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Of the Contact Cathartics, which acts on BOTH the LI and SI
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Castor Oil (Other just act on LI)
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Hydrolyzed in the upper SI to form Ricinoleic acid
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Castor Oil
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May cause a brown pigmentation of the colonic mucosa (melanosis coli)
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Anthraquinones (Contact cathartic)
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May cause dehydration and uterine contractions
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Castor Oil
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Reduces plasma ammonia concentrations in the plasma (useful in tx protal-systemic encephalopathy) and also > water and electrolye concentrations in the colon
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Lactulose
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Nonabsorbed sugar that is met by olonic bacteria, producing severe flatulence, cramps and ab discomfort
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Lactulose
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SE of all osmotic lax (but esp Sodium Phosphate)
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intravascular volume depletion and electrolyte imbalances (hypokalemia) and should be used with caution in pts with sig cardiac disease!
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MOA of Lubiprostone
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activates chloride channel ClC2 to increase liquid secretion
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Selective u receptor antagonists that do not cross the BBB (Misc cathartics)
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Alvimopan, Methylnaltrexone
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Lubiprostone is used to tx what?
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chronic, idiopathic constipation and constipation-predominant IBS
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Used in pts receiving palliative care (long term) as a cathartic
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Methylnatrexone
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Used to shorten period of postoperative ileus following small or large bowel resection (cathartic)
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Alvimopan (Short term!)
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SE of Alvimopan
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cardiotoxicity (hence only short term use in hospitalized pts!)
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