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177 Cards in this Set

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  • Back
What do parietal cells secrete?
HCl and IF
What do G cells secrete?
Gastrin
Where does somatostatin come from?
D cells
In the gut, epithelial cells secrete what substances?
mucus and HCO3-
Pepsinogen comes from what cells?
chief cells
How does Acid regulation occur in the stomach and GI?
through endocrine, paracrine and autocrine methods
If you disrupt acid secretion, what could result?
ulcers
What is the cause of a cushing ulcer?
tramua
What is the cause of a curling ulcer?
severe burns
What are general causes of ulcers?
increased # of parietal cells
high serum gastrin levels
loss of acid-mediated neg feedback
rapid gastric emptying
H. Pylori infection
NSAIDS
smoking/alcohol
GERD
Decreased mucus/HCO3-
What is zollinger-ellsion syndrome?
gastrin producing tumor in the pancreas--usually is malignant
What are some symptoms of an ulcer?
abdominal pain, nausea, vomiting (vomiting blood), bloody stool, indigestion, weight loss, fatigue
How do antacids help with Ulcers?
They neutralize the acid
What are some examples of antacids?
sodium bicarbonate(gas), calcium carbonate (gas, renal insufficiency), magnesium hydroxide (osmotic diarrhea), aluminum hydroxide (constipation and CNS toxicity)
What are H2 antagonist?
They bind competitively to H2 receptors on histamine cells.

They are highly selective for histamine cells and inhibit 60-70% of 24hr acid secretion
What is the common ending for H2 blockers?
-tidine
What are adverse effects of H2 blockers?
CNS effects
endocrine effects
hepatic P450 metabolism
What are common side effects of H2 blockers?
diarrhea, headache, fatigue, constipation, infection

With IV infusion: Bradycardia and hypotension
How long do H2 blockers last?
10-6 hrs
Why are PPIs so efficacious?
The inhibit the final common pathway for acid secretion

Require the synthesis of a new pump in order to secrete HCl again
In what pH are PPIs activated?
low phH
What is the common ending for PPIs?
-prazole
What are other ways that you could protect the lining of the stomach from acid, other than decrease acid production?
increase mucosal production
What does sucralfate do?
adheres to ulcer and creates a physical barrier

Also stimulates mucus secretion
What is another tx that is similar to sucralfate?
bismuth subsalicylate
What does bismuth subsalicylate do besides creating a physical barrier and increasing mucus production?
kills bacteria
How does Misoptostol protect the stomach?
It stimulates PGE1 receptors
What is a common negative effect with bismuth subsalicylate?
blackening of the tongue and stools

In high doses can cause salicylate toxicity
What are common adverse effects of misoprostol?
cramping and diarrhea.

Can also cause abortificient
What are common adverse effects of sucralfate?
constipation, impaired drug absorption

Need to be careful with rena insufficient pts
If you have a renal insufficient pt who presents with an ulcer--what mucosal protective agent should you NOT give?
sucralfate
Bismuth subsalicylate treats what?
dyspepsia, diarrhea and H. pylori infection
Sucralfate treats which type of ulcer?
duodenal ulcer
misoprostol treats which type of ulcer?
NSAIDS induced
How is H Pylori transmitted?
orally through fecal matter and it can be transmitted from the stomach to the mouth through gastro-esophageal reflux or belching.
Does H. Pylori alone cause ulcers?
no
What is the 1st line of defense in H. Pylori ulcers?
New Triple Therapy:
PPI
Clarithromycin
Amoxicillin or metronidazole
What was the old defense in treating H. Pylori ulcers?
Bismuth subsalicylate
tetracycline
metronidazole
What is the quadruple therapy with treating H. Pylori?
Bismuth subsalicylate
PPI
clarithromycin
amoxicillin or metronidazole
How do prokinetic agents stimulate GI Motility?
Acts on:

Serotonin rececptor 4 to increase motility
What effect does Serotonin have on GI motility?
It stimulates the 5-HT4 receptors on cells to release ACh on GI smooth muscle--GI contraction
What effect does Dopamine have on GI motility?
Stimulates D2 receptors to inhibit GI motility
What receptor does Cisapride stimulate?
5-HT4 receptor agonist
What receptor does Metoclopromide stimulate?
5-HT4 receptor agonist and D2 receptor antagonist
What receptor does Bethanechol stimulate?
Muscarinic receptor agonist
What receptor does erythromycin stimulate?
motilin receptor agonist
What receptor does Neostigmine stimulate?
AChEI
What is Neostigmine use to treat?
Bowel obstruction
What are the negative side effects of neostigmine?
Cholinergic side effects
What is bethanechol used to treat?
GERD
What are the negative side effects?
cholinergic side effects
What is Cisapride used to treat?
GERD, impaired gastric emptying
What are negative side effects of Cisapride?
Diarrhea, seizure and cardiac arrhythmias
What is metoclopramide used to treat?
GERD
impaired gastric emptying
What are the negative side effects of metoclopramide?
fatigue
insomnia
altered motor function
Parkinsonian symptoms
What is erythromycin used to treat?
impaired gastric emptying
What are the negative side effects of erythromycin?
erythromycin mediated side effects
What are laxatives used to treat?
constipation (infrequent or difficult)
What is the first way the pt should try to treat constipation?
increase water intake
increase fiber intake
increase exercise
What are the different categories of laxatives?
bulk-forming
stool softeners
osmotic
stimulant
wheat bran, methylcellulose and metamucil are common types of what laxative?
bulk-forming
What is the route of administration of bulk-forming laxatives?
oral
How do bulk-forming laxatives work?
The form a gel like substance in the intestines that increases in diameter. The increase in diameter triggers peristalsis in the gut.
Name two types of stool softeners
glycerin
mineral oil
Stool softeners can be administered how?
oral or rectal
How does glycerin work?
penetrates stool and allows water and lipids to penetrate as well
How does mineral oil work?
coats stool with oil to allow for easier passage.
What are osmotic laxatives?
induce change in osmotic pressure with non-absorbable sugars and salts.
How are osmotic laxatives administered?
oral or rectal
Name some common osmotic laxative agents?
Milk of magnesia
sorbitol
lactulose
PEG (polyethylene)
How do stimulant laxatives work?
stimulation of ENS
inducing a leaky mucosa
inhibiting sodium uptake by the gut
Name some common stimulant laxatives
Anthraquinone
castor oil
diphenylmethane (phenophthalein)
Name two derivatives of anthraquinone.
senna and aloe
How does castor oil work?
it stimulates smooth muscle contraction
What are the routes of administration for stimulant laxatives?
rectal and oral
What is an adverse side effect of bulk forming laxatives?
gas
When are laxatives used?
constipation
minimize straining
prior to surgical and endoscopic procedures
What is an adverse side effect of osmotic laxative?
gas
electrolyte flux
What is an adverse side effect of stimulant laxative?
mucosal surface damamge
What is an adverse side effect of surfactant?
nutrient malabsorption
When treating diarrhea, first you should deal with what?
treat underlying cause first:
infection
inflammation
osmotic diarrhea (lactose intolerance)
secreting tumors
What are common anti-diarrheal agents?
opioids
bismuth compounds
kaolin and pectin
bile salt resins
octreotide
Why do opioids used in tx of diarrhea not cause CNS effects?
they do not cross the BBB
What is the administration route for opioids?
oral
What is the MoA for opioids?
decrease peristaltic contractions
increase segmental (mixing) contractions
increase internal anal sphincter tone
decrease perception of GI distension
Which part of bismuth subsalicylate mediates the anti-diarrheal effects?
salicylate inhibition of prostaglandin synthesis
What is kaolin?
magnesium aluminum silicate
What is pectin?
non-digestible sugar found in apples
What do pectin and kaolin do?
The absorb water and bacterail toxins in the gut
How are kaolin and pectin administered?
orally
name some examples of bile salt binding resins
cholestyramine
colestipol
How does cholestyramine and colestipol contribute to antidiarrheal effects?
bind bile salts in the gut that are present due to mal-absorption. (seen in crohn's disease or resection of the ileum)
What do bile salts do to the lumen?
increase osmotic pressure in the lumen (influx of water)
What is octreotide?
A peptide similar to somatostatin--acts as an agonist to somatostatin receptor
How is octreotide administered?
IV or SC
Name two opioids that are used as antidiarrheal agents.
Loperamide
diphenoxylate
What is loperamide used for?
Loperamide is used for IBS diarrhea
What are the side effects of loperamide?
Constipation.

A very safe agent
What are the uses for diphenoxylate?
diarrhea
What are the adverse side effects of diphenoxylate?
CNS effects
atropine effects
What is B.P used for?
non-specific diarrhea
traveler's diarrhea
What are some adverse effects of B.P?
salicylate toxicity
What are some common adverse side effects of kaolin
constipation
What is kaolin used for?
diarrhea
What is cholestyramine used for?
impaired bile-salt absorption mediated diarrhea
What are adverse effects of cholestyramine?
bloating, flatus, constipation, fecal impaction, impaired fat absorption
What is octreotide used for?
secretory diarrhea
What is an adverse effect of octreotide?
tachyphylaxis and unwanted somatostatin effects
How can an emetic response be initiated?
sensory stimulation (CTZ)
blood-borne emetics
gastrointestinal irritants
Where is the emetic center located?
medulla
Regulation of the emetic response is under what transmittors?
serotonin
dopamine
histamine
ACh (muscarinic)
What sites are useful in suppression of the emetic response?
GAGAergic neurons (benzodiazepenes)
cannabioid receptors glucocorticoid receptors opioid receptors
What type of mechanism does Ondansetron use?
5-HT3 antagonist
When is ondansetron used?
Chem/radiation induced nausea and vomiting
What are some adverse effects of ondansetron?
headache
dizziness
constipation
prolonged QT interval
What method does scopolamine use in its antiemetic effect?
M1 antagonist
What are adverse effects of scopolamine?
antimuscarininc effects
When do you use scopolamine?
motion sickness
What method does metoclopramide use to prevent emetic reactions?
It is a D2 antagonist
Metoclopramide is used in what cases?
chemo/radiation induced nausea and vomiting
What are the adverse effects of metoclopramide?
GI motility, Parkinsonian symptoms
What methods does Dimenhydrinate use to prevent an emetic effect?
It is an H1 antagonist
When would you use dimenhydrinate?
motion sickness
What drugs would you use with motion sickness?
dimenhydrinate
scopolamine
What are the adverse effects of dimenhydrinate?
drowsiness
What are the adverse effects of lorazepam?
drowsiness
What anti-emetic drugs cause drowsiness?
lorazepam
dimenhydrinate
When would you use lorazepam?
anxiety
chemo/radiation
What methods does Tetrahydrocannabinol use to decrease emetic effects?
cannabinoid agonist.
What are the adverse effects of tetrahydrocannabinol?
sedation
hypotension
drowsiness
dry mouth
ataxia
When would you use tetra-hydrocannabinol?
chemo/radiation nausea/vomiting
When would you use prednisone?
chemo/radiation nausea/vomiting
What is the MoA of prednisone?
glucocorticoid agonist
What are the adverse effects of prednisone?
weight gain
water retention
What is the best therapeutic strategy to treat IBS?
relieve pain and improve bowel function
In treatment of IBS, what are common strategies?
loperamide (reduce diarrhea)
osmotic laxatives (constipation)
tricylic antidepressants (relieve pain)
What agents are currently being used to treat IBS?
serotonin
What is the method of action of alosetron
5-HT3 antagonist
What is the predominant cause of use of Alosetron in pt with IBS?
diarrhea-predominant IBS in women
What are adverse effects of Alosetron?
constipation
ischemic colitis
What is the MoA of Tegaserod?
5-HT4 agonist
When is tegaserod used?
in constipation-predominant IBS in women
What are some adverse effects of Tegaserod?
diarrhea
headache
cardiovascular
(was recently removed from the US market)
There are three types of agents used to treat IBD. Name them.
Aminosalicylates
glucocorticoids
purine analongs
anti-TNF alpha antibodies
What is aminosalicylates MoA?
inhibition of IL-1, TNFa, NF-xB, COX and free radical scavenging
What is the MoA of glucocorticoids?
suppression of multiple inflammaotry processes
(cytokine production)
What is the MoA of purine analogs?
inhibition of immune cell proliferation
What is the MoA of anti-TNFa antibodies?
inhibition of tumor necrosis factor a mediated immune response
Where do 5-ASA work?
topically, not systemically
5-ASA is mostly absorbed where?
80% is absorbed in the duodenum
Olsalazine, balsalazide and sulfasalazine target what area?
colon
Mesalamine-pentasa targets what area?
throughout intestines
Mesalamine-asacol targets what area?
ileum/proximal colon
What is the only 5-ASA that is not administered through an oral route? And which route is it administered?
mesalamine-rowasa and Canasa

enema or suppository
Sulfasalazine, balsalazide and olsalazine are modified where?
Azo bond linked
N(triple bond)N
Mesalamine-pentasa is modified how?
time release microgranules
mesalamine-asacol is modified how?
pH sensitive resin
Mesalamine-rowasa and canasa is modified how?
high concentrations
Mesalamine-rowasa and Canasa target what areas?
rectum/sigmoid colon
Name the glucocorticoids.
prednisone
prednisolone
hydrocortisone
budesonide
What are the routes of administration for glucocorticoids?
IV
oral
suppository
What is the mechanism of action of glucocorticoids?
suppresses TNFa, IL-1 (inflammatory cytokines)
suppresses IL-8 (chemokines)
suppresses adhesion molecules
supresses signal transduction that mediate cytokine and chemokines activities (NOS, PLA2, COX2, NF-xB)
Name the three agents of antimetabolites?
6-mercaptopurine
azathioprine
methotrexate
What are the routes of administration of antimetabolites?
IM
SC
oral
What is the MoA for antimetabolites?
inhibition of purine synthesis

results in decreased DNA synthesis adn repair, which leads to decreased cell proliferation
What is sulfasalazine used for?
Ulcerative colitis
What are the adverse effects of sulfasalazine?
nausea/GI upset
arthralgia
myalgia
bone marrow suppression
malaise
What is mesalamine used for?
UC
Crohn's disease
What are the possible side effects of mesalamine?
very safe
rare nephritis
What are the adverse effects of prednisone?
weight gain
water retention
When would you use prednisone?
moderate to severe active IBD
When would you use Azathioprine?
maintenance of remission of IBD (onset 17 wks)
What are adverse side effects of azathioprine?
nausea
vomiting
bone marrow suppression
What are the adverse effects of Methotrexate?
low dose make side effect uncommon:

include bone marrow depression
When do you use Methotrexate?
maintenance of remission of Crohn's (onset 8-12wks)
What are the adverse effects of infliximab?
infection
When would you use Infliximab?
severe crohn's disease