module 3 antiemetics Flashcards
patho of emesis
midbrain contains high concentrations of emetogenic receptors
- dopamine D2 receptors
- muscarininc-cholinergic
- histamine
- 5HT3
Rx with affinity for dopamine receptors
antagonize dopamine
- benzamides
- butyrophenones
- phenothiazines
5HT3 antagonist
highly bound to 5HT3 receptors both centrally and peripherally
corticosteroids
dexamethasone
- prevent chemotherapy induced N/V
anticholinergics
block cholinergic muscarinic receptors
antihistamines
act directly on the vomiting center and vestibular pathways
phenothizaine drugs
chlorpromazine
prochlorperazine
promethazine
- cheap, inc. AE, dec. efficacy
phenothiazine receptor site affinity
D2: ++++
muscarinic-cholinergic: ++
histamine: +++
serotonin: +/-
butyrophenones
droperidol
haloperidol
butyrophenones receptor site affinity
D2: ++++
muscarininic-cholinergic: -
histamine: +
serotonin: +/-
benzamides
metoclopramide:
promote gut motility
gastroparesis
corticosteroids
bethamethasone
dexamethasone
anticholinergic
scopolamine
meclizine
- motion sickness
anticholinergic receptor site affinity
D2: +
muscarininc-cholinergic: ++++
histamine: +
serotonin: -
antihistamines
cyclizine
hydroxyzine
diphenhydramine