Anti Emetic & Motility Flashcards
Vomiting center location
Ill-defined
In the medulla oblongata, consists of tractus solitarius and parts of reticular formation
Neurotransmitters involved in NV
Substance P
Acetylcholine
Y-aminobutyric acid
Cannabinoids
Serotonin
Dopamine
Chemoreceptor trigger zone
Highly vascular
Lacks true blood brain barrier-direct stimulation of circulating toxins
Communicates with vomiting center via D2 and 5-HT3 receptors
PONV factors
Women/non-smokers/hx of motion sickness
Length of procedure/type of procedure
Inhaled anesthetics, nitrous, opioids, neostigmine
Serotonin receptor antagonists (5-HT3)
Competitive antagonism of 5-HT3 receptors- very specific and free of neurological effects
Not effective for Motion induced NV
CYP450 and renal elimination
Ex Ondansetron
Ondansetron
Therapeutic after 30-60 min-typically given on induction
Half-life 4 hours
Adult 4-8mg
QTc
Granisetron and Dolasetron
Similar to zofran
Double the half-life- typically used in chemo
Palonosetron
Most effective 5-HT3 antagonist
40hr half-life…
Not used in anesthesia!! But fda approved for chemo
Dopamine receptor antagonists
Dopamine receptor blocker in the CNS-blocks adenylate cyclase to reduce cAMP….
Avoid in Parkinson’s
Increase EPS
Serotonin cascade
Serotonin is released from enterochromaffin cells of small intestine
- vagal afferents stimulated via 5-HT3 receptors
-initiates vomiting reflex.
Dopamine antagonist ex
Droperidol- QTc… eeek
Haloperidol (butyrophenone)-
Metoclopramide (benzamide)- antiemetic and prokinetic via GI cholinergic mechanisms
Corticosteroids MOA
Synthetic glucocorticoid with anti inflammatory properties
Elusive
Decreases serotonin release
Acts on glucocorticoid receptors in vomiting center
Primarily dexamethasone is given 4-8mg
Dexamethasone considerations
Perineal itching in awake patients
2 hour onset
Combine with 5-ht3
Transient hyperglycemia-careful in diabetics
And avoid in acute leukemia due to tumor lysis syndrome
Neurokinin-1 receptor antagonists
Competitive antagonism with substance P at central GPCRs (NK receptors)
Aprepitant
Only NK-1 approved by FDA
50% reduction in NV
PO only 40mg preop
Well tolerated w/out QTc