Anti-emetics Flashcards
What are the steps in emesis ?
- nausea, salivation and sweating
- retrograde peristalsis
- deep inspiration
- closure of glottis
- adbo muscles contract
- LOS relaxes
what make the chemical trigger zone activate ?
Sensory afferents via midbrain
direct triggers
vestibular nuclei
visceral afferents from gut
what drugs act on the vestibular nuclei ?
Muscarinic receptor antagonists
H1 receptor antagonists
Name 1 Muscarinic antagonist / anti-spasmodic drug
hyoscine hydrobromide
how does hyoscine hydrobromide work ?
what are its uses/benefits ?
competitive blockade of M ACh receptors (nonspecific) in vestibular nuclei and CTZ
People who cant take tablets
motion sickness
bowel obstruction
what are the side effects of hydroscine hydrobromide ?
sedation
memory problems
glaucoma
dry mouth and constipation
How do H1 receptor antagonists work ?
acts on vestibular nuclei by inhibiting Histaminergic signals from vestibular system to the CTZ in medulla
name 3 H1 receptor antagonists
Cyclizine - not suitable for elderly or children Levomepromazine Clinnirazine promethazine diphenhydramine
what are side effects of clinnirazine ?
H1 antagonist
Sedation , excitation , Antimuscarinic (dry mouth, constipation, urinary retention)
cardiac toxicity
what agents act on visceral afferents in the gut ?
5HT3 receptor antagonists
D2 Receptor antagonists
where is serotonin produce in the gut ?
what is it stimulated by ?
what is the effect of serotonin on the Gut ?
enterochromaffin cells parasympathetics SM contraction = increases motility Increases gut secretions regulates appetite
What are the main functions of 5ht3 Receptor antagonists ?
centrally- inhibits the CTZ
Peripheral - reduces GI motility / secretions
name 2 5HT3 antagonists
Ondansetron , Granesitron and palonosetron
1st line treatment
what are the side effects of Ondansetron ?
uncommon
Constipation , headache , elevated LFTs, long QT syndrome , dystonia , parkinsonism
name a D2 receptor antagonist specific to viscreal afferent of the guts
Metacloperamide
domperidone
how does Metaclopramide work ?
increase ACh at M receptors in Gut =
promotes gastric emptying by:
Increasing tone at LOS and amplitude of gastric contractions
decrease tone of pylorus = increased peristalsis
what are D2 antagonists used for ?
GORD , ileus
what are the side effects of metaclopramide ?
Galactorrhoea via prolactin release
Dystonia , parkinsonism
what is domperidone alternative use ?
what is its main side effect?
improving lactation for mothers
sudden cardiac death
what drugs act on the CTZ ?
5HT3 receptor antagonists H1 antagonists Muscarinic antagonists D2 . antagonists Corticosteroids cannabinoids NK1 antagonists
name 2 anti psychotics/ d2 antagonists
Haloperidol
Levomepromazine
chlorpromazine
Prochlorperazine
what D2 antagonists is used in pregnancy ?
prochlorperazine
what is haloperiodol used for ?
chemotherapy and palliative care