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69 Cards in this Set

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  • Back
  • 3rd side (hint)
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?
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
vision disturbance
(careful in narrow-angle glaucoma!)
What nausea drugs are antihistamines?
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
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
What is the most common side effect of meclizine?
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
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?
Due to QTc prolongation, promethazine should not be given with what other drugs?
type Ia antiarrhythmics (quinidine)
all FQs
What are the ADRs of promethazine?
tardive dyskinesia
What are the three categories of dopamine antagonists?
Name a phenothiazine (pure D2 activity)
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?
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?
Dec Libido
What are the dystonias associated with use of dopamine antagonists?
carpopedal spasm
tongue protrusion
how are dopamine antagonist induced dystonias treated?
d/c drug and give diphenhydramine
Name a butyrophenone.
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?
Name 2 benzamides.
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?
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)
metoclopramide (a benzamide)
What drug for N/V is antagonized by anticholinergics?
What N/V drug has dose related drowsiness and acute dystonia as side effects (but probably no SEs at hospital dosages)?
Name 3 first generation seratonin antagonists.
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?
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.
What is the most common side effects with seratonin antagonists?
Which two seratonin antagonists may have QT prolongation issues?
dolasetron and palonsetron
Which drug for N/V is a substance P antagonist?
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?
Which antiemetic also is an appetite stimulant? (hint: not used very often)
Which two CIE drugs are better for delayed N/V?
aprepitant and palonsetron