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69 Cards in this Set

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  • Back
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Where is the motor function of the gut controlled?
1. sympathetic and parasympathetic
2. enteric brain neurons
3. smooth muscle cells
what kind of acid-base abnormality is likely to result from N/V?
metabolic alkalosis
What are the 3 primary pathways involved in stimulating the vomiting center in the CNS?
1. vestibular fibers
2. visceral fibers
3. chemoreceptor trigger zone (in 4th ventricle)
Which 5 NT receptor sites are important in vomitting reflex?
muscarinic, histamine, dopamine, 5HT3 (seratonin), and NK1 (substance P)
Where does scopolamine work?
blocks acetylcholine parasympathetic sites in
1. smooth muscle
2. secretory glands
3. CNS
Which types of nausea is scopolamine effective for?
vestibular system is rich in histamine and ACH so scopolamine is good for motion sickness (but not so much for visceral causes)
What anti-nausea drug is an anticholinergic?
scopolamine (M1)
What anti-nausea drug is a muscarinic antagonist?
scopolamine
What is an indication for use of scopalamine besides N/V?
to dry oropharyngeal secretions in order to decrease chance of aspiration
What two drugs have overlapping toxicities with scopolamine?
other anticholinergics and other CNS depressants
What are the main adverse drug reactions of scopolamine?
dry mouth
sedation
vision disturbance
(careful in narrow-angle glaucoma!)
What nausea drugs are antihistamines?
diphenhydramine
dimenhydrinate
meclizine
promethazine (H1 AND D2)
How does diphenhydramine work?
competes with histamine for receptor sites on effector cells (in GI tract, blood vessels, and respiratory tract)
What are the clinical indications for use of diphenhydramine or dimenhydrinate?
motion sickness
OTC sleep aid
Allergies
What is the problem with using diphenhydramine for allergies?
allergic disease is persistent and pt will not adjust to sedation
What are the two most common SEs of diphenhydramine or dimenhydrinate?
sedation and xerostomia
How does dimenhydrinate work?
competes with histamine for receptor sites on effector cells (in GI tract, blood vessels, and respiratory tract)
the same as diphenhydramine
How does meclizine work?
- blocks CTZ (central anticholinergic)
- decreases excitability of middle ear labyrinth
- blocks conduction in middle ear vestibular-cerebellar pathways
What are the two major indications for the use of meclizine?
motion sickness
vertigo
What is the most common side effect of meclizine?
sedation
same as dimenhydrinate w/o xerostomia
What is the difference between promethazine and other antihistamines?
is is a phenothiazine derivative; it is an antagonist at both H1 and D2 receptors; it is used as adjunct pain management
How does promethazine work?
blocks postsynaptic mesolimbic dopaminergic receptors in the brain
- alpha adrenergic blocking --> depresses release of hypothalamic/hypophyseal hormones
- competes with histamine for receptor
What are the clinical indications for use of promethazine?
motion sickness
antiemetic
adjunctive for pain management
What are the CYP interactions of promethazine? What drug should it not be given with?
2D6 substrate; SSRIs
What antiemetic should be avoided in patients taking levodopa?
promethazine and other phenothiazines
What drug for motion sickness/emesis is contraindicated in kids <2 because of potentially fatal respiratory depression?
promethazine
Due to QTc prolongation, promethazine should not be given with what other drugs?
type Ia antiarrhythmics (quinidine)
TCAs
all FQs
What are the ADRs of promethazine?
EPS
NMS
tardive dyskinesia
amenorrhea/gynecomastia
What are the three categories of dopamine antagonists?
phenothiazines
butyrophenones
benzamides
Name a phenothiazine (pure D2 activity)
prochlorperazine
How do phenothiazines work?
block postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain (including CTZ)
What type of CIE might prochlorperazine be effective for?
mild-moderate
What type of N/V will phenothiazines NOT be effective for?
vestibular disorders
highly emetogenic chemo
Which dopamine antagonist does not cause QTc prolongation?
Benzamides (metoclopramide, trimethobenzamide)
What are the major ADRs of phenothiazines?
dystonias
EPS
Amenorrhea
Gynecomastia
Galactorrhea
Dec Libido
Agranulocytosis
Hyperactivity
What are the dystonias associated with use of dopamine antagonists?
torticollis
opisthotonos
carpopedal spasm
trismus
tongue protrusion
how are dopamine antagonist induced dystonias treated?
d/c drug and give diphenhydramine
Name a butyrophenone.
droperidol
how does droperidol work?
block postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain (including CTZ)
same as phenothiazines
what are the common clinical indications for use of droperidol?
preanesthetic for procedural sedation

post-op N/V
Which N/V drug has a black box warning about QTc prolongation?
Butyrophenones (droperidol)
Why do you have to be careful about using droperidol with furosemide or thiazides?
may induce hypokalemia
What dopamine antagonist may lead to NMS?
droperidol
butyrophenone
Name 2 benzamides.
Metoclopramide
Trimethobenzamide (no better than placebo)
How do benzamides work?
cause central and peripheral D2 receptor antagonism

At high doses they block 5HT receptors in the CTZ

Enhance response to ACH in UGI tissue
Which Dopamine antagonist is prokinetic?
Benzamides (metoclopramide)
Explain the prokinetic property of metoclopramide.
enhances motility without stimulating gastric, biliary, or pancreatic secretions.
what dopamine antagonist may be used for diabetic gastroparesis?
metoclopramide
What type of CIE might metoclopramide be used to treat?
mild-moderately emetogenic regimens
What two dopamine antagonists may be used for mild-moderate emetogenic CIE?
prochlorperazine (a phenothiazine)
and
metoclopramide (a benzamide)
What drug for N/V is antagonized by anticholinergics?
metoclopramide
What N/V drug has dose related drowsiness and acute dystonia as side effects (but probably no SEs at hospital dosages)?
metoclopramide
Name 3 first generation seratonin antagonists.
ondansetron
granisetron
dolasetron
If the first dose of ondansetrone doesn't work what do you do? what about metoclopramide?
switch drugs; inc dose of metoclopramide
What is the second generation seratonin antagonist? What is the advantage?
palonsetron - higher affinity for receptor; longer half life
Which seratonin antagonist is only available IV?
palonsetron
What drugs can be prescribed for nausea related to irradiation?
seratonin antagonists
Ondansetron is a _______ substrate but it is such a clean drug this interaction doesn't really matter.
3A4
What is the most common side effects with seratonin antagonists?
headache
Which two seratonin antagonists may have QT prolongation issues?
dolasetron and palonsetron
Which drug for N/V is a substance P antagonist?
aprepitant
How does aprepitant work?
selectively inhibits neurokinin 1 receptor --> blocking substance P
What two drugs should aprepitant be combined with for the best prevention of acute and delayed CIE?
dexa and a 5-HT3 antagonist
What are the CYP interactions of substance P antagonists?
substrate of 3A4
Dexamethasone is an effective antiemetic in what situation?
mild-moderately emetogenic chemo (and as a component for highly emetogenic regimens)
What is the MOA of dexamethasone for prevention of emesis?
who knows?!
Which antiemetic is a synthetic delta-9-tetrahydrocannabinol?
dronabinol
Which antiemetic also is an appetite stimulant? (hint: not used very often)
dronabinol
Which two CIE drugs are better for delayed N/V?
aprepitant and palonsetron