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97 Cards in this Set

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