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Pharm 2 Final - GI Drugs
Drugs used to treat GI disorders
130
Health Care
Graduate
05/01/2009

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Cards

Term
Which drugs are cytoprotective?
Definition

Sucralfate

Misoprostol

Arthrotec

Term
what is arthrotec?
Definition

a combination of diclofenac (an NSAID) and misoprostol

 

treats arthritis and prevents possible NSAID assc. ulcers

Term
what do cytoprotective drugs do?
Definition
they protect the GI mucosa
Term
Sucralfate is a polymer of...
Definition
sucrose and aluminum hydroxide
Term
how does sucralfate protect the GI mucosa?
Definition

it adheres to the ulcer crater and prevents its contract with gastric acid

 

it also stimulates PG synthesis which provides protection

 

all of this allows the ulcer to heal

Term
how often do you take sucralfate?
Definition
4xs/day - 1 gram tablets
Term
sucralfate PK
Definition

PO (tablet or liquid)

essentially no absorption

Term
what is sucralfate indicated for?
Definition

active PUD

 

suppress recurrences of ulcers

Term
sucralfate SEs
Definition
mild GI sxs
Term
How is misoprostol cytoprotective?
Definition
its a PG analogue that inhibits gastric acid secretion while promoting the secretion of mucous and bicarb
Term
Misoprostol SEs
Definition

diarrhea, and other GI complaints

 

contraindicated in pregnancy, can stimulate uterine contractions

Term
why would you use misoprostol?
Definition
to prevent NSAID-induced ulcers only
Term
Is diarrhea is disease or disorder?
Definition
no, its a sxs of a GI disorder
Term
Most cases of diarrhea only need _____ to treat it.
Definition
time
Term
Causes of diarrhea
Definition

infection

maldigestion

inflammation

functional disorders of the bowel

Term
Diarrhea definition
Definition
characterized by stools of excessive volume and fluidity, and by increased frequency of defecation
Term
what are the most serious complications associated with diarrhea?
Definition

dehydration

and

depletion of electrolytes

Term
management of diarrhea is directed at:
Definition

Dx and Txt of underlying d/o

replacement of lose water and salts

relief of cramping

reducing the passage of unformed stools

Term
antidiarrheal drugs fall into which 2 groups?
Definition

1. specific antidiarrheal drugs

 

2. nonspecific antidiarrheal drugs

Term
what do specific antidiarrheals treat?
Definition
the underlying causes of diarrhea
Term
what do nonspecific antidiarrheals treat?
Definition
the symptoms of diarrhea
Term
Nonspecific antidiarrheal drugs
Definition

opiods (diphenoxylate + aropine, Loperamide, Paregoric)

 

bulk forming agents (attapulgite, polycarbophil)

 

Bismuth Subsalicylate

 

antispasmodics

Term
how do opioids help with diarrhea?
Definition

they stimulate the opioid receptors in the GI tract and suppress peristalsis and thereby facilitate absorption of water and electrolytes

 

this reduces the fluidity and volume of stools and the frequency of defecation

Term
why is dependence not really an issue when opioids are prescribed for diarrhea?
Definition
bc the dose is low
Term
why is diphenoxylate combined with atropine?
Definition
it is included to discourage abuse
Term
what is the only indication for diphenoxylate?
Definition
diarrhea
Term
loperamide is a structural analog of...
Definition
meperidine
Term
why do you not see opioid like SEs from using loperamide for diarrhea?
Definition
bc it is poorly absorbed and does not readily cross the BBB
Term
which opioid used for diarrhea is really only prescribed for babies?
Definition
Paregoric (Schedule III)
Term
how does attapulgite help with diarrhea?
Definition
it pulls diarrhea-causing substances from the digestive tract, also provides bulk
Term
how does polycarbophil (fibercon) help with diarrhea?
Definition
it gives the stool a more firm, less watery consistency
Term
how does bismuth subsalicylate help with diarrhea?
Definition

it decs the secretion of fluid into the intestine

 

 

Term
how does bismuth help treat PUD?
Definition

1. forms a protective coating over the ulcer crater

 

2. promotes secretion of bicarb and PGs

 

3. suppresses growth of H. pylori

Term
how do antispasmodics help with diarrhea?
Definition
the can relieve cramping assc with diarrhea but they do not alter fecal consistency or volume
Term
how long should you use antidiarrheals?
Definition
only a couple of days
Term
what do laxatives do?
Definition
they stimulate intestinal peristalsis and inc. movement of contents through the bowel
Term
why would you prescribe/use laxatives?
Definition

- to treat constipation

 

- to evacuate the bowel prior to surgery or dx procedures

 

- to purge the system of poisons

Term
Laxative Effect:
Definition
refers to the production of a soft, formed stool over a period of one or more days (mild)
Term
Catharsis:
Definition
when evacuation of bowel is fluid and prompt (intense)
Term
what is the primary cause of constipation?
Definition
poor diet - a diet deficient in fiber and fluids
Term
what 2 ways does fiber facilitate colonic function?
Definition

1. some types absorb water, thereby softening the feces and increasing  the mass

 

2. other types are digested by colonic bacteria, whose subsequent growth increases fecal bulk

Term
which drugs can be used as an adjunct to antihelmintic therapy?
Definition
laxatives
Term
what are the different types of laxatives?
Definition

bulk forming

surfactants

contact agents

saline laxatives

 

glycerin

lactulose

mineral oil

polyethylene glycol

Term
what is the MOA of bulk forming agents used as laxatives?
Definition
absorb water and increase the mass in the GI tract. The mechanical distention stimulates peristalsis
Term
which are the safest of all laxatives?
Definition

bulk forming agents

 

methylcellulose (citrucel)

Psyllium (metamucil)

bran

Term
what do you need to tell patients to do when they take bulk forming agents?
Definition
to take with a full glass of water
Term
which drugs are surfactant laxatives?
Definition

docusate sodium

docusate sodium + casanthranol

docusate calcium

docusate calcium + casanthranol

Term
what is the MOA of surfactant laxatives?
Definition

decrease surface tension on stool and allow water to penetrate and soften the contents

 

(almost like a soap)

Term
MOA of contact agent laxatives
Definition

stimulants irritate the intestinal mucosa and increase intestinal motility

 

also alter electrolyte and fluid absorption

Term
surfactant laxatives containing sodium should be used in caution in which patients?
Definition
those with CHF
Term
which drugs are contact agent laxatives?
Definition

senna - senakot

cascara sagrada

phenolphthalein - exlax

bisocodyl - dulcolax

castor oil

Term
which laxatives are most often abused?
Definition
contact agents
Term
MOA of saline laxatives
Definition
produce an osmotic effect in the intestinal lumen that causes fluid accumulation, intestinal distention and peristalsis
Term
saline laxatives
Definition

Magnesium hydroxide - MOM

magnesium sulfate - epsom salts

magnesium citrate - citrate of Mg

Sodium Phosphate - phospho-soda

sodium biphosphate + sodium phosphate - fleets enema

Term
SEs of saline laxatives
Definition
fluid and electrolyte alterations
Term
how does glycerin help with constipation?
Definition
it pulls water from the extraluminal spaces into the feces and stimulates reflex evacuation
Term
how is glycerin usually admin'ed?
Definition
via suppositories
Term
which laxative is good for infants and children?
Definition
glycerin
Term
What is the major use of Lactulose?
Definition

to reduce ammonia levels in liver dysfunction

(by 25-50%)

Term
As a laxative, Lactulose __________ into the intestinal lumen making the stool softer.
Definition
pulls water
Term
Is lactulose a safe laxative?
Definition
yes, because its bascially not absorbed
Term
How does mineral oil act as a laxative?
Definition
it lubricates the feces and the intestinal mucosa preventing water from being resorbed from the feces
Term
Mineral oil is used to treat constipation and maintain soft stools when _____________ is contraindicated.
Definition
straining
Term
How can you administer mineral oil?
Definition
PO or by enema
Term
Mineral oil can impair the absorption of what other medications? And what can you do to prevent this?
Definition

fat soluble vitamins

oral contraceptives

anticoagulants

 

you can stagger the doses so its not an issue

Term
List the SEs of Mineral Oil.
Definition

N/V/D, abd cramping

Anal irritation, pruritis ani, infection

aspiration pneumonia

 

may soil underwear :(

Term
When is polyethylene glycol used?
Definition
for patients who are about to have some procedure, like a colonscopy
Term
If emesis is secondary to motion sickness, what might you prescribe?
Definition

antihistamines (dramamine)

Anticholinergics

benadryl

Term
If emesis is due to a "central cause" you might prescribe...
Definition

Phenothiazine

Cannabinoid

Metoclopramide

Term
How do Phenothiazines help treat emesis due to a "central cause"?
Definition

they inhibit dopaminergic transmission at the CTZ

 

they also inhibit stimulation of the vagus nn (which innervates the stomach)

Term
List the phenothiazines.
Definition

Promethazine - Compozine

Prochlorperazine - Phenygrin

Term
Metoclopramide inhibits ______________ at the CTZ, and improves gastric ______________ .
Definition

dopaminergic transmission

 

emptying

Term
Which drugs are good to give a person suffering from emesis due to chemotherapy?
Definition
Serotonin receptor antagonists
Term
List the serotonin receptor antagonists.
Definition

Ondansetron - Zofran

Granisetron - Kytril

Dolasetron - Anzemet

Term
Serotonin receptor antagonists antagonize the serotonin receptors found on the _________________ and in the ________.
Definition

vagal nerve terminals

 

CTZ

Term
What are the 3 major causes of PUD?
Definition

1. H. Pylori

2. Increased Acid Secretion

3. Inadequate Mucosal Defense vs. Gastric acid

Term
Based on the 3 major causes for PUD, what needs to happen to each to treat them?
Definition

1. Eradicate H. Pylori

2. Decrease secretion of HCl or neutralize HCl

3. Protect gastric mucosa

Term
Which drugs eradicate H. Pylori?
Definition

Metronidazole (Flagyl)

Amoxicillin

Clarithromycin

Tetracyclin

Bismuth

 

Use in combinatino for 2 weeks

Term
Treating H. Pylori results in a ______ cure rate with low recurrence rates.
Definition
90%
Term
Bismuth Subsalicylate inhibits _________ and increases the secretion of _____________. It has an ________________ effect too.
Definition

pepsin

 

mucus

 

antibacterial

Term
What are the receptors types found parietal cells that stimulate acid secretion?
Definition

histamine

Cholinergic

CCK-B receptors for gastrin

PG receptors

Term
Which drug groups inhibit acid secretion?
Definition

Histamine2 Receptor Antagonists

Proton Pump Inhibitors

Muscarinic Receptor Antagonists

 

Term
List the Histamine2 Receptor Antagonists.
Definition

Cimetidine - tagamet

Ranitidine - Zantac

Famotidine - Pepcid

Nizatidine - Axid

Term
Histamine2 Receptor Antagonists block these receptors to inhibit ________________. (MOA)
Definition
acid secretion
Term

Ranitidine and Famotidine decrease the _________, ___________ and _____________ secretion of gastric acid.

Definition

basal

 

food-stimulated

 

nocturnal

Term
H2RAs have a minimal effect on gastric acid secretion induced by _______ and _____________.
Definition

PSNS

 

parasympathomimetics

Term
H2RAs are indicated for:
Definition

1. Peptic Ulcers

2. GERD

Term
With continued use of H2RAs, receptor production is ______________ and patients become tolerant to them.
Definition
down-regulated
Term
Why is Cimetidine not recommended?
Definition
Because it has so many drug interactions
Term
Which H2RA is the most potent?
Definition
Famotadine - Pepcid
Term
H2RAs are absorbed well ________.
Definition
orally
Term
Which H2RA is the best one, but it has just not caught on?
Definition
Nizatadine (Axid)
Term
Which is the only H2RA that does not have metabolites that are excreted renally?
Definition
Nizatadine - Axid
Term
Name the PPIs
Definition

Omeprazole - Prilosec

Lansoprazole - Prevacid

Rabeprazole - Aciphex

Pantoprazole - Protonix

Esomeprazole - Nexium

Term
PPIs bind to and irreversibily inhibit the __________ of the parietal cells, resulting in a marked decrease in _______________.
Definition

H/K -ATPase pump

 

acid secretion

Term
Why is tolerance not a problem with PPIs?
Definition
since new proton pumps are continuously being synthesized
Term
PPIs produce a dose dependent inhibition of up to ________% of gastric acid secretion.
Definition
90-95%
Term
A single PPI dose can inhibit acid secretion for _________.
Definition
1-2 days
Term
PPIs inhibit ________ and _________ gastric acid secretion.
Definition
basal and stimulated
Term
Which drugs would be good to use to treat hypersecretory states like ZE syndrome?
Definition
PPIs
Term
PPIs must be administered as ______________ or _________________ because they are unstable in the presence of acid.
Definition

enteric coated preparations

or

buffered suspensions

Term
What is Prevacid Naprapac?
Definition

a combination of Lansoprazole and naproxen

 

(Naproxen may not produce ulcers in this combination)

Term
_____________ (a PPI) effects are decreased by cigarette smoking.
Definition
Pantoproazole - Protonix
Term
Which PPI is extensively metabolized by CYP2C19 and 3A4, but does not have any clinically significant interactions with warfarin, quinidine or phenytoin?
Definition
Esomeprazole - Nexium
Term
PPIs are indicated for treatment of:
Definition

PUD

GERD/Erosive gastritis

Hypersecretory Syndromes

Term
Muscarinic Receptor Antagonists are mos often prescribed for _____________.
Definition
"nervous stomach"
Term
List the muscarinic receptor antagonists
Definition

Dicyclomine

Glycopyrrolate

Phenobarbital + hyocyamine + atropine

 

(these are antispasmodics)

Term
Muscarinic receptor antagonists are considered _________________.
Definition
second line
Term
Which different agents neutralize stomach acid?
Definition

Magnesium Hydroxide - MOM

Aluminum Hydroxide

Calcium Carbonate + Simethicon

Sodium Bicarbonate

Term
Absorption of antacids is neither ___________ nor ____________.
Definition
necessary nor desired
Term
What are the commonly used cations in antacids?
Definition

magnesium

calcium

Aluminum

Term
What is the most common anion used in antacids?
Definition
Hydroxide
Term
What problems can occur if antacids are absorbed?
Definition

hypermagnesium in pts with renal failure

 

acid-base abnormalities

Term
Antacids have a _________ onset of action?
Definition
quick
Term
Which antacids have the 1st and 2nd fastest onsets of actions?
Definition

1. Sodium Bicarb

2. Mg Hydroxide

Term
Why is Sodium Bicarbonate not used much as an antacid anymore?
Definition
because of its high sodium content
Term
What is the duration of action of antacids?
Definition

If taken on an empty stomach = 1 hr

 

If taken after a meal = 3 hr

Term
Why are frequent doses of antacids required?
Definition
because of their short duration of action
Term
With antacids, anions combine with the ___________________ secreted by the stomach to form ______, thereby increasing the _____ of the stomach contents. (MOA)
Definition

acidic hydrogen cations

 

water

 

pH

Term
Antacids only increase stomach pH to _____ but this neutralizes about _____ of the gastric acid.
Definition

4-5

 

90%

Term
Antacids are as effective as any other drug therapy for PUD, but what is the catch?
Definition
pH must be kept at 3.5 to 4.0 throughout each 24 hour period, so you need to take about 200 cc/day. (about 7 times a day)
Term
Antacids are used to treat:
Definition

PUD

GERD
Acid Indigestion

Prevent Stress ulcers

Term
Why would you combine Aluminum hydroxide with Magnesium hydroxide?
Definition

because they offset their SEs

 

Aluminum Hydroxide - constipation

Mg Hydroxide - diarrhea

 

Maalox, Mylanta etc.

Term
How do antacids cause drug interactions?
Definition

by interfering with the absorption of other drugs administered at the same time

 

by binding with them

 

or by changing their transit time

Term
List the SEs of Antacids
Definition

Diarrhea/Constipation

 

hypermagnesium characterized by hypotension, N, V, EKG changes, mental depression and coma

 

Calcium - "milk-alkali syndrome"

Term
Which drugs increase GI motility?
Definition

Prokinetic agents

(Metoclopramide)

Term
What might cause decreased motility?
Definition

systemic disease

intrinsic Gi problem

medications

Term
Which GI drug has a new black box warning?
Definition
Metoclopramide
Term
Metoclopramide is usually dosed ___ or ___ for ____________________
Definition

tid or bid

 

chronic gastroparesis

Term
List the SEs of Metroclopramide
Definition

Insomnia

Parkinsonian effects/dystonias

galactorrhea and menstral disorders (stimulates prolactin release)

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