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1 Emesis
Scammell
60
Pharmacology
Graduate
04/26/2010

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Cards

Term
where is the emetic center, CTZ, and area postrema?
Definition
floor of the 4th ventricle in the caudal medulla
Term
the emetic center is accessed by what?
Definition
both CSF and blood
Term
emetic center receives inputs from?
Definition
multiple sites
Term
the area postrema is outside of what?
Definition
BBB
Term
area postrema controls what?
Definition
vomiting

inputs from a variety of places
Term
4 inputs to the area postrema?
Definition
1. blood-borne stimulants
2. solitary taste inputs
3. vestibular inputs
4. vagal afferents
Term
what is responsible for the coordination of the physiological response of vomiting?
Definition
DMX
Term
what is the role of DMX in vomiting?
Definition
responsible for the physiological response of vomiting
Term
5 emetics?
Definition
1. apomorphine
2. vestibulation
3. ipecac
4. chemo
5. radiation
Term
5 receptor types on the CTZ?
Definition
1. opioid
2. D2
3. H1
4. muscarinic
5. 5HT3
Term
what receptors on the CTZ are for vestibular inputs?
Definition
H1 and muscarinic
Term
what receptor on the CTZ is for vagal afferent input?
Definition
5HT3 receptors
Term
what is the NT between the CTZ and emetic center?
Definition
substance P
Term
3 inputs directly to the emetic center?
Definition
1. higher centers for vision, taste, thought, etc
2. vagal input
3. gut distention
Term
3 categories of anti-emetics?
Definition
1. 5HT3 antagonists
2. H1/muscarinic blockers
3. neurokinin receptor blockers
Term
which type of anti-emetic is best for chemo induced vomiting?
Definition
5HT3 antagonists
Term
what is a 5HT3 antagonist used as an anti-emetic during chemo?
Definition
ondansetron
Term
what type of anti-emetic inhibits vestibular input?
Definition
H1/muscarinic blockers
Term
3 H1/muscarinic blockers used as anti-emetics?
Definition
1. dimenhydrinate
2. promethazine
3. scopolamine
Term
what type of anti-emetic is aprepitant?
Definition
neurokinin receptor blocker - inhibits substance P
Term
substance P blockers is useful in blocking emesis from what inputs?

what inputs would they NOT be useful in blocking?
Definition
useful in blocking emesis from activation of opioid, dopamine, serotonin, and muscarinic receptors

not useful for emesis induced by inputs of sensation from higher centers (vision, taste, though), vagal input, or gut distention
Term
2 drugs that induce emesis?
Definition
1. syrup of ipecac
2. apomorphine
Term
admin of syrup of ipecac?
Definition
given orally, OTC
Term
mechanism of syrup of ipecac?
Definition
local irritant in the intestine

also has direct effect on CTZ
Term
onset of emesis with syrup of ipecac?
Definition
15-30 mins
Term
syrup of ipecac should only be given to what types of patients?
Definition
conscious
Term
onset of apomorphine?
Definition
acts more rapidly
Term
mechanism of apomorphine?
Definition
direct effects of CTZ
Term
why are syrup of ipecac and apomorphine not administered routinely in the management of poisoned patients?
Definition
they may counteract the efficacy of other, more effective treatments such as activated charcoal, oral antidotes, and whole-bowel irrigation
Term
3 more effective treatments than emetic drugs in the management of poisoned patients?
Definition
1. activated charcoal
2. oral antidotes
3. whole-bowel irrigation
Term
3 5HT3 receptor antagonists?
Definition
1. ondansetron
2. granisetron
3. palonosetron
Term
use of 5HT3 receptor antagonists?
Definition
alone or in combination for chemo-induced nausea and hyperemesis of pregnancy
Term
adverse effects of 5HT3 receptor antagonists?
Definition
1. well tolerated
2. constipation
3. headache
Term
2 dopamine D2 receptor antagonists?
Definition
1. promethazine
2. metoclopramide
Term
promethazine also blocks what receptors (besides D2)?
Definition
1. cholinergic
2. histaminergic
Term
therapeutic use of dopamine D2 receptor antagonists?
Definition
1. gastroenteritis
2. drug induced nausea
3. motion sickness
Term
adverse effects of dopamine D2 receptor antagonist?
Definition
1. drowsiness
2. diarrhea
3. extra-pyramidal effects
Term
anti-histamines used as anti-emetics are antagonists at which receptor?
Definition
H1
Term
what other activity do anti-histamines have (besides H1)?

why are they important?
Definition
1. anti-muscarinic
2. anti-cholinergic

leads to side effects
Term
3 anti-histamines?
Definition
1. dimenhydrinate
2. dipehnhydramine
3. meclizine
Term
therapeutic uses of anti-histamines?
Definition
motion sickness
Term
adverse effects of anti-histamines?
Definition
sedation
dry mouth
Term
how does scopolamine work?
Definition
its a muscarinic receptor antagonist
Term
what is the drug of choice anti-cholinergic used as an anti-emetic?
Definition
scopolamine
Term
how is scopolamine administered?
Definition
in patches
Term
therapeutic use of scopolamine?
Definition
motion sickness - used prior to motion
Term
adverse effects of scopolamine?
Definition
1. drowsiness
2. dry mouth

b/c of muscarinic blocking effects
Term
dronabinol is what type of drug?
Definition
cannabinoid
Term
how is dronabinol administered?
Definition
available orally
Term
therapeutic use of dronabinol?
Definition
1. prophylactic agent in cancer chemo
2. appetite stimulant in patients with AIDS or anorexia
Term
adverse effects of dronabinol?
Definition
central sympathetic stimulation leading to tachycardia
Term
what happens upon withdrawal of dronabinol?
Definition
irritability and insomnia
Term
what glucocorticoid is used as an anti-emetic?
Definition
dexamethasone
Term
therapeutic use of dexamethasone?
Definition
anti-nausea drug in patients with widespread cancer
Term
how does dexamethasone work as an anti-nausea drug?
Definition
through its anti-inflammatory activity and decreased PGE secretion
Term
adverse effects of dexamethasone?
Definition
typical effects of parenteral corticosteroids --> hypoglycemia and mood changes
Term
what is a substance P/NK1 receptor antagonist used as an anti-emetic?
Definition
aprepitant
Term
what type of drug is aprepitant?
Definition
substance P/NK1 receptor antagonist
Term
therapeutic use of aprepitant?
Definition
used in combo with dexamethasone and a 5HT3 receptor antagonist for acute and delayed emesis a/w cancer chemo

pre-treatment for chemo --> effective regardless of type of chemo they are undergoing
Term
adverse effects of aprepitant?
Definition
tiredness
constipation
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