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GI Pharm > N/V tx > Flashcards

N/V tx Flashcards

1
Q

receptors in area postrema

chemoreceptor trigger zone

A

D2
NK1
5HT3

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2
Q

receptors in nucleus tractus solitarius

vomiting center

A

H1
M1
NK1
5-HT3

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3
Q

receptors in stomach

A

chemoreceptors
mechanoreceptors
5-HT3
signals transmitted to vomiting center via IX or X

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4
Q

receptors in vestibular system

A

M1

maybe H1

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5
Q

5-HT3 receptor antagonists

A 
Dolasetron
granisetron
ondansetron (Zofran)
palonosetron 
alosetron (only for IBS-D)
Block 5-HT3 receptor at vagal nerve
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6
Q

Therapeutic use of 5-HT3 antagonists

A

CINV
RINV
post operative N/V
Pregnancy N/V

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7
Q

adverse effects of 5-HT3 antagonists

A

QT prolongation and Torade’s
caution when used with antiarrhythmics
- dolasetron very high risk!
headache and constipation

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8
Q

Pharmacokinetics of 5-HT3 antagonists

A

Palonosetron and Granisetron have long half-lives
effective for delayed CINV as single dose
all others have short half-lives

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9
Q

Neurokinin (NK1) antagonists

A

aprepitant
fosaprepitant
netupitant (combo only with palonosetron)
rolapitant

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10
Q

MOA of NK1 antagonists

A

block NK1 receptors in CTZ and vomitting center

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11
Q

therapeutic use of NK1 antagonists

A

CINV in combo with glucocorticoids and 5-HT3 antagonists
prophylaxis of post operative N/V
- only aprepitant and fosaprepitant

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12
Q

adverse effects of Nk1 antagonists

A

GI distress

CNS effects, fatigue

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13
Q

pharmacokinetics of NK1 antagonists

A

netupitant/rolapitant have longer half lives and oral routes

inhibition of several CYP450 enzymes

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14
Q

H1 antagonists

A 
diphenhydramine (benadryl)
dimenhydrinate (dramamine)
hydroxyzine
promethazine
meclizine 
cyclizine
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15
Q

H1 antagonists MOA

A

weak antiemetics
useful for post-operative N/V
block H1 receptors in vomiting center and vestibular system
also have central anticholinergic properties!!!

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16
Q

Therapeurtic uses of H1 antagonists

A 
mild N/V 
PONV
pregnancy N/V (doxylamine/B6)
motion sickness (meclizine and cyclizine) 
CINV
RINV
17
Q

adverse effects of H1 antagonists

A

anticholinergic effects!!!

18
Q

pharmacokinetics of H1 antagonists

A

hydroxyzine has long half life

interactions include other anticholinergic agents pt may be on

19
Q

D2 antagonists

A 
Phenothiazine's 
- chlorpromazine
- perphenazine
- prochlorperazine 
metoclopramide
20
Q

D2 antagonists effects

A

weak to moderate antiemetic
block D2 in cortex
metoclopramide stimulates Ach actions in GI enhancing motility

21
Q

Therapeutic use of D2 antagonists

A 
idiopathic, mild N/V (infections, opiates, migraines)
Metoclopramide for gastroparesis 
PONV
NVP 
CINV and RINV in combo with other agents
22
Q

Adverse effects of D2 antagonists

A

classic anticholinergic effects

arrhythmias possible with larger doses

23
Q

interactions of D2 antagonists

A

other anticholinergic agents
antiarrhythmics (QT prolongation)
anti-hypertensives

24
Q

M1 antagonists

A

scopolamine
weak antiemetic for motion sickness
block ach signaling from vestibular nuclei to VC
adverse effects include classic anticholinergic effects

25
Q

cannabinoid agonists

A

dronabinol (CIII)
nabilone (CII)
strong antiemetics for treatment resistant CINV
stimulates central CB1 and peripheral CB2 receptors in VC and CTZ
reduces 5-HT3 release from vagal afferents
also increases appetite in anorexic cancer or AIDS pts
short onset time and long duration of action

26
Q

adverse affects of cannabinoid agonists

A 
irritability 
vertigo
sedation
impaired cognition
xerostomia 
sympathomimetic
27
Q

interactions of cannabinoid agonists

A

caution with CNS depressants, CV agents, and sympathomimetics

28
Q

High emetogenic regimen for CINV

A 
NK1 antagonist (aprepitant)
5-HT3 antagonist
Dexamethasone 
give 1 day prior and 3 days after chemo 
add cannabinoid in treatment resistant
29
Q

Moderate emetogenic regimen for CINV

A 
5-HT3 antagonist (palonosetran/granisetran)
dexamethasone 
give day before and 2 days after chemo 
add NK1 antagonist if necessary 
add cannabinoid in treatment resistant
30
Q

Low emetogenic regimen for CINV

A 
Dexamethasone or
5-HT3 antagonist or
metoclopramide or
prochlorperazine 
give day prior to chemo
31
Q

Pregnancy induced N/V stepped therapy

A

B6 + doxylamine (H1) or 5-HT3 antagonist
D1 antagonist
Steroid or different D1 antagonist

GI Pharm (6 decks)

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