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Terms in this set (111)
cholinergic, adrenergic, serotonergic, dopaminergic, GABA-ergic
what are all the receptors that affect the GI tract?
autonomic (parasympathetic primarily)
what innervates GI tract?
the Gi tract in influenced by numerous hormones, including ____ hormones that are produced in the GI tract itself
acid, bicarbonate, mucous, water, paracrine, autocrine, and endocrine hormone
GI tract secretions:
gastroesophageal reflux, gastritis, peptic ulcer disease, gastric ulcer disease
what are your acid peptic disorders
protective of the gastric epithelium, produce mucous and bicarbonate, stimulated by protective prostaglandins
what do mucous producing cells do?
produce gastrin in response to different stimuli: food in stomach, calcium, other hormones
what do gastrin cells do?
produce acid in response to various stimuli
what do parietal cells do?
increase intracellular calcium, which activates specific kinases that stimulate the hydrogen/potassium ATPase system that ultimately secretes acid into the stomach lumen
gastrin and acetylcholine act through their receptors to do what?
histamine is secreted by what cells?
stimulates the hydrogen/potassium pump via adenylyl cyclase/cAMP second messenger system
histamine that acts as a paracrine hormone to do what?
gastrin, CCK, Acetylcholine, other neurotransmitters
ECL cells are stimulated by what?
drugs that are used to neutralize acid once it is produced and secreted into the stomach
antacids do not affect what?
reduce the symptoms (pain) related to excess acid production
main effect of antacids
when used alone, aluminum hydroxide has what affect that causes them to be used in conjunction with another agent?
aluminum hydroxide is poorly absorbed, so most of their effect is in what?
some magnesium is absorbed, so use with caution in what disease?
strong laxative effect
magnesium has a strong what effect?
magnesium and aluminum
most of the clinically useful antacids are a combination of both ___ and ___ compounds, so each counteracts the adverse effect of the other
what can result in elevated calcium levels
gastrin secretion, rebound hyperacidity
calcium stimulates ___ ___, causing a ___ ___
these agents are associated with a large sodium load that may be detrimental in renal failure, heart failure, and HBP
constipation and diarrhea, increased gastrin production, increased sodium load, drug interactions
adverse effects of antacids
many drugs are absorbed by the charged metal ions in antacids in a process known as ____
forming a protective gel that provides a coating over ulcers that promotes healing and prevents further erosion
sucralfate polymerizes in the stomach, forming what?
can cause constipation, oral only, must be taken several times a day (reducing patient compliance)
systemic effects of sucralfate
they mediate inflammation, and are the receptors blocked by traditional antihistamine drugs.
what are the H-1 receptors jobs?
what type of receptors are the subtype of histamine agents found n the GI tract
parietal cell acid production, and traditional antihistamines do not affect acid peptic disorders
H-1 receptors are not involved in what?
Cimetidine, Famotidine, Ranitidine, and Nizatidine
H-2 blocking drugs:
parietal cell H-2 receptors
H-2 blocking drugs competitively inhibit what?
basal and nocturnal acid secretion
H-2 blocking drugs decrease what two things?
blockade of H-1 receptors
these drugs are selective for H-2 receptors and do not cause what?
decrease gastric acid secretion
H-2 blocking drugs only real clinical effect is to do what?
reduce the symptoms in all types of acid-peptic disease, accelerate ulcer healing, prevent recurrences of gastric and duodenal ulcers, and decrease the symptoms of gastroesophageal reflux
what are the clinical uses of H-2 blockers
all the H-2 blockers are now available _____
H/K ATPase (the proton pump) is located in the pica membrane of the __ ___ along the secretory canaliculi
Omeprazole (prototype), Lansoprazole, Esomeprazole, Pantoprazole, Rabeprazole
specific proton pump inhibitors
All PPIs are weak bases. Diffuse into the canaliculi of the parietal cell. Become acidified, and cannot diffuse out. Concentrated in the parietal canaliculus, where they form covalent bonds with,
and irreversibly inactivate the proton pump. Result is profound reduction of gastric acid. PPIs are all highly protein bound. May displace other drugs, or be displaced by other drugs, altering pharmacokinetics. Plasma half life of 1 to 2 hours. However, they have a long duration of action due to concentration in parietal
Mechanism of Action of proton pump inhibitors
elevate pH significantly
PPIs as a group do what?
Peptic ulcer disease (PUD), Gastric ulcers, H. Pylori induced gastritis
NSAID associated ulcers and gastritis, GERD, Zollinger-Ellison syndrome
Clinical uses of PPIs
increased gastrin production
PPIs may result indirectly in __ __ ___ due to loss of acid inhibition of gastrin producing cells
diarrhea, headaches, abdominal pain, hypergastrinemia, decreased bioavailability of drugs that require an acid stomach environment, increased risk of infection
adverse effects of PPIs
chronic helicobacter pylori
what infection is present in most patient with recurrent non-NSAID induced ulcers and gastritis
3 antibiotics plus a PPI
H. Pylori regimens all include at least what?
motility disorders frequently involve what?
diabetic neuropathy, parkinson disease, multiple system atrophy
motility disorders are often the result of what kinds of autonomic neuropathies?
nausea, bloating, dyspepsia, and severe gastroesophageal reflux
motility disorders are characterized by delayed stomach emptying, with what resultant symptoms?
facilitating the effect of acetylcholine
in the GI tract, metoclopramide appears to exert its effect by what?
what is the parasympathetic neurotransmitter in the GI tract
increases GI tract motility
increasing acetylcholine activity does what?
hasten gastric emptying and decreases gastroesophageal reflux by increasing lower esophageal sphincter tone
what is the net effect of metoclopramide
usefulness of metoclopramide is limited by its what?
severe dystonic disorders, tardive dyskinesia, hyperprolactinemia
what symptoms occur when dopamine blockade occurs in the CNS?
serotonin agonist (5-HT4) receptors
cisapride binds to what receptors?
prolongs that QT interval and leads to cardiac arrhythmias (tornado de points) especially when used with other drugs that affect the QT
adverse effects of cisapride
binds motilin receptors and mimics the action of motilin. antimicrobial, chronic use can lead to antibiotic resistant organisms
use of erythromycin
another dopamine antagonist. not approved for use in USA, but widely used elsewhere for gastroparesis and nausea. can at times by obtained when no other alternative are available
use of domperiodone
large intestinal motility disorders usually involve conditions of ____ motility
dicyclomine, belladonna, and hyoscyamine
decrease GI motility
anticholingeric agents do what?
used for constipation-predominant irritable bowel syndrome and idiopathic chronic constipation
prostaglandin analog used for constipation and cramping in IBS
new prostaglandin agent, works similarly to Lubiprostone
these are the most effective drugs for diarrhea control
decrease GI motility and decrease GI secretions
as a group, opioids do what two things?
morphine, codeine, paregoric
the most effective drugs for diarrhea control, CNS effects and abuse potential limit usefulness
opioids with only minimal or weak CNS effect (do not cross BBB). usually combined with atropine to minimize abuse risk
use of diphenoxylate
only minimal or weak CNS effects. safer and is available over the counter
use of loperamide
magnesium silicate (clay) and soluble fiber combination
use of kaolin/pectin
especially useful in diarrhea associated with increased bile acid secretion such as the Dumping syndrome that may be seen after cholecystectomy
use of cholestyramine and colestipol
newer agent recently approved for diarrhea dependent IBS. blocks serotonin type 3 receptors in the GI tract. black box warning due to increased risk of ischemic colitis
use of alosetron
inhibits D2 receptors in the chemoreceptor trigger zone in the medulla. may also affect serotonin specific (5-HT3&4) receptors. useful for nausea from chemotherapy, post-op nausea, malignancy, uremia, and others. also effective for treating migraines.
use of metoclopramide
use of metoclopramise if limited by what?
extrapyramidal effects. dopamine blockade occurs in the CNS: severe dystonic disorders, tradeoff dyskinesia, hyperprolactinemia
adverse effects of metoclopramide
also a dopamine antagonist. chemically and pharmacologically related to the typical antipsychotic agents. indications for use are similar to metoclopramide
use of prochlorperazine
sedation and EPS
adverse effects of prochlorperazine
diphenhydramine, meclizine, and promethazine
anti-emitics: antihistamines (H1 antagonists)
H1 and acetylcholine receptors antagonists. appear to exert their action in the medullary CTZ. useful in treating nausea, vomiting, and vertigo. very sedating, often used as hypnotics
use of antihistamines (H-1 antagonists)
dry mouth, decrease lacrimation, extrapyramidal effects (especially promethazine)
adverse effects of antihistamines (H-1 antagonists)
ondansetron, granisetron, and dolasetron
serotonin 5-HT3 antagonists
CNS effects on serotonin receptors in the medullary CTZ. also have effects on peripheral nerves and GI tract serotonin receptors. especially effective for chemotherapy induced nausea and post-op nausea. no effect on vertigo
use of ondansetron, granisetron, and dolasetron
constipation, headache, QT prolongation and cardia arrhythmias
adverse effects of serotonin antagonists
dronabinal, nabilone, and medical marijuana
complex CNS effects. inhibits chemoreceptors trigger zone probably by endocannabinoid mediated pathways, but exact mechanism unknown.
use of cannabinoids
___ are used to promote passage of stool in those cases requiring treatment
patients on prolonged bedrest, with painful or very infrequent bowel movements, spinal cord injuries affecting stool passage, those who must avoid straining at stool, for bowel cleansing prior to surgery or diagnostic procedures
laxatives are definitely indicated for:
lactulose, polyethylene glycol, magnesium hydroxide, magnesium citrate
used to promote passage of stool in those cases requiring treatment. increase water in the bowel through osmotic action. increase stool volume. increase bulk. soften stool. improved peristaltic action. fairly safe, often used for acute constipation and for bowel cleansing because they are so effective.
use of osmotic agents
magnesium overdose can occur especially in patients with impaired renal function
adverse effects of osmotic agents
psyllium, methylcellulose, dietary soluble fiber
fairly safe. similar to osmotic agents in that they provide bulk to the stool, increase water in the stool, and facilitate passage of larger but softer stool
use of bulk agents
bisacodyl and senna
affect the intestinal mucosa and/or the enteric plexus to stimulate peristalsis. potentially harmful, especially if used long term
use of bisocodyl and senna
has proven to be particularly useful in treating the severe constipation that occurs with long term opioid use
use of senna
anionic surfactant that increases water content of stool with resultant stool softening. do not use with mineral oil because it emulsifies oil and leads to its absorption form the intestine. rarely used for acute constipation, more useful as a preventive for long term use
use of docusate
not absorbed, passes readily and rapidly through the GI tract. simply lubricates the stool bolus to allow better passage through the GI tract.
use of mineral oil
if aspirated, it can lead to lipoid pneumonia. can affect the absorption of fat soluble nutrients. should not be used with anionic surfactants like decussate, because they can emulsify mineral oil and allow it to be absorbed systemically
mineral oil has the potential for possible harm in several different ways:
prostaglandin analog. chloride channel activator. increases stool water content
tell me about lubiprostone:
affect GI motility via 5-HT4 receptors in the enteric plexus. tegaserod no longer available in USA
tegaserod affects what?
in emergency or life threatening situations due to increased risk of cardiac events and stroke
tegaserod no longer available in USA except in what?
used for treating steatorrhea caused by chronic pancreatitis or other causes of inadequate pancreatic enzyme secretion.
use of pancrelipase
budesonide and hydrocortisone
mesalamine and sulfasalzine
release 5-aminosalicylic acid locally into the GI tract, with subsequent anti-inflammatory effects similar to ASA and NSAIDS.
use of anti-inflammatories
what is a component of sulfasalazine that is responsible for most of anti-inflammatories adverse effects:
azathioprine, mercaptopurine, infliximab
inhibit TNF, leukocytes, and various other components of the immune system
use of immunosuppressant agents
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