Tx of N/V Flashcards
N/V receptors include
serotonin 5-HT (setron) Neurokinin (pitant) Histamine H1 Dopamine D2 Muscarinic M1 (scopalamine) cannabinoid receptors (dronabinol nabilone)
in addition to antagonists/agonists to a bunch of receptors, what agents are used in the tx of N/V
glucocorticoids such as dexamethasone
benzodiazepines such a alprazolam/lorazepam
serotonin receptor antagonsists
setron dolasetron granisetron ondansetron palonosetron
IV only 5-ht antagonist
palonosetron (all others have PO/IV)
unique 5-ht antagonist in its indicaiton
alosetron is only indicated for IBS-D
5-ht receptor antagonists are indicated for
CINV RINV PONV NVP STRONG antiemetic agents block 5-HT receptors at CTZ from intestinal enterochromaffin cells
AE of 5-ht antagonists
CNS -HA
GI - constipation/diarrhea (Serotonin syndrome)
WORST POSSIBLE AE
Dose-dependent QT prolongation and Torsade’s
use extreme caution when using with other QT prolonging agents
longest lasting 5-HT antagonists
palonosetron and sutstained SQ granisetron
effective for delayed CINV as a single dose
drug interactinos for 5-HT receptor antagonsits
QT prolonging agents
Antiarrhythmics
NK1 receptor antagonists include
aprepitant (and fosaprepitant)
netupitant (and fosnetupitant)
rolapitant
MoA of NK 1 receptor antagonists
block substance p (neurokinin 1) receptors in CTZ/VC
peripheral blockade of NK1 receptors located on vagal terminals in gut maybe too
moderate antiemetic agents
unique indication of aprepitant
PONV
given up the 3 hours prior to anesthesia
-pitants are most effective when given with
a glucocorticosteroid and 5-ht3 antagonist
AE of NK1 antagonsits
gi - dyspepsia/constipation/diarrhea
cns - dizziness/fatigue/somnolence
H1 receptor antagonists
diphenhydramine dimenhydrinate hydroxyzine promethazine meclizine cyclizine
unique indication for doxylamine (h1 receptor antagonist)
prepared with b6 (pyridoxine)
INITIAL THERAPY FOR NVP
PO only h1 receptor antagonists
meclizine
cyclizine
dramamine (dimenhydrinate, generic is IV/IM as well)
indications for H1 receptor antagonists as it relates to N/V
PONV
block histamine type 1 receptors in VC and vestibular system
huge consideration for h1 blockers
exhibit anticholinergic effects drowsiness dry mouth constipation urinary retention blurred vision decreased BP
therapeutic uses of h1 receptor antagonsits
idiopathic/mild n/v PONV NVP motion sickness/vertigo (meclizine and cyclizine) CINV/RINV add on therapy
unique indication for meclizine and cyclizine
motion sickness/vertigo
D2 receptor antagonists
phenothiazines (chlorpromazine, perphenazine, prochlorperazine)
other (metoclopramide, haloperidol, olanzapine, trimethobenzamide)
D2 receptor antagonist MoA
weak-moderate antiemtic agents
block dopamine 2 recpetors in CTZ
unique MoA of metoclopramide
stimulates Ach actions in GI, enhancing GI motility and increasing LES tone
no impact on GI secretion