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o Cardiovascular: serotonin
o Nervous System:
Serotonin: stimulates itch and pain sensory nerve endings.
Clinical Pharmacology:
o Serotonin Agonists
generally mild
altered sensations (tingling, warmth, etc.)
dizziness
muscle weakness
neck pain
Chest pain (frequency: 5%)
o Contraindications:
o Serotonin Antagonists
Cyproheptadine
Ketanserin Ritanserin
(Periactin)
Ondansetron Granisetron
Tropisetron Dolasetron
(Zofran) (Kytril)
Cyproheptadine (Periactin)
o Overview
Ondansetron (Zofran)
o 5-HT3 receptor blocker
Surgical patients:
3% increased liver transaminase enzyme levels
3% headache
No sedation, hypotension, dysphoria, extrapyramidal reactions --
side effects associated with other antiemetic drugs
Tropisetron:
o 5-HT3 receptor blocker
Granisetron (Kytril)
o More selective 5-HT3 receptor blocker compared to ondansetron
o Clinical Use:
Dolasetron:
o Highly potent/selective 5-HT3 receptor blocker
o Clinical Use:
Serotonin
Chemistry: serotonin
o Widely distributed indoleethylamine formed from L-tryptophan:
storage or
rapid inactivation-- oxidation (monoamine oxidase, MAO)
Pineal gland: serotonin -- precursor for melatonin (melanocyte-
stimulating hormone)
o Storage:
Most serotonin (> 90%):enterochromaffin cells -- GI tract
Blood: platelets (active carrier-mediated transport system
{similar to nerve endings})
CNS locations:serotonin
raphe nuclei (brain stem)
localization of neuronal cell bodies that:
A. synthesize
B. store
C. release
CNS serotonin involvement:
mood
sleep
appetite
temperature regulation
pain perception
blood-pressure regulation
vomiting
o Degradation:
cAMP, potassium
Raphe nuclei,
5-HT1A channels:partially
hippocampus
selective agonist: 8-OH-
DPAT
cAMP,partially
5-HT1D(a,b) brain selective agonist:
sumatriptan (Imitrex)
receptor:Na-K ion
channel: partially
area postrema, sensory selective antagonists
5-HT3
and enteric nerves ondansetron (Zofran),
ggranisetron (Kytril),
tropisetron
cAMP; partially
5-HT4 CNS, ,smooth muscle
selective agonists:
metoclopramide (Reglan)
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