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Cards (63)
What are the primary storage sites for serotonin?
Enterochromaffin cells
and
platelets
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What is one of the central nervous system effects of serotonin?
Mood regulation
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How does serotonin affect blood pressure?
It
regulates
blood pressure
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What role does serotonin play in temperature regulation?
It helps regulate body temperature
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How does serotonin influence pain perception?
It acts as a
stimulant
for pain perception
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What is one of the peripheral effects of serotonin?
Vasoconstriction
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What are the types of serotonin receptors?
5HT1A
5HT1B/1D
5HT2A
5HT2C
5HT3
5HT4
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Where is the 5HT1A receptor located?
CNS
in
presynapse
of neurons
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What effect does the 5HT1A receptor have on serotonin release?
It
decreases
the
release
of
serotonin
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What is the coupling type of the 5HT1B/1D receptor?
Gi
coupled
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Where is the 5HT1B/1D receptor located?
Peripheral smooth muscles
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What effect does the 5HT1B/1D receptor have?
It causes
contraction
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What is the coupling type of the 5HT2A receptor?
Gq
coupled
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What effect does the 5HT2A receptor have?
It causes
vasoconstriction
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Where is the 5HT2C receptor located?
CNS
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What effect does the 5HT2C receptor have?
It
reduces
appetite
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What type of channel is the 5HT3A receptor?
Ligand gated ion channel
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Where is the 5HT3A receptor located?
Area of
postrema
of
CTZ
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What effect does the 5HT3A receptor have?
It induces
vomiting
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What is the coupling type of the 5HT4 receptor?
Gs
coupled
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Where is the 5HT4 receptor located?
GIT
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What effect does the 5HT4 receptor have?
It promotes
peristalsis
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What are the uses of 5HT1A receptor drugs?
Partial agonist in the brain
Used as an
anti-depressant
Example:
Buspirone
(BuSpar)
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What are the uses of 5HT1B/1D receptor drugs?
Agonists
for acute migraine and cluster headache
Examples:
Sumatriptan
,
Naratriptan
,
Zolmitriptan
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What is the prototype drug for 5HT1B/1D receptor?
Sumatriptan
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What is the duration of action for Sumatriptan?
2-3
hours
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How is Sumatriptan metabolized?
By
MAOA
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What are the side effects of 5HT1B/1D receptor drugs?
Coronary vasospasm
and
paresthesias
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What are the uses of 5HT2A receptor drugs?
Partial agonists
for acute migraine and cluster headache
Examples:
Ergotamine
,
Dihydroergotamine
(DHE)
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What is the best route for Ergotamine administration?
Rectal
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What is the risk associated with ergots?
Rebound headache
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What is the effect of Dexfenfluramine?
Reduces appetite for
weight control
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What are the uses of 5HT3 receptor antagonists?
Management of chemotherapy-induced nausea and vomiting (
CINV
)
Examples:
Ondansetron
,
Granisetron
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What is the route for Palonosetron administration?
Single
IV
dose for
5-7
days
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What are the uses of 5HT4 receptor drugs?
Management of Irritable Bowel Syndrome (
IBS
) and
GERD
Examples:
Tegaserod
,
Cisapride
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What are eicosanoids?
Important group of
endogenous
fatty acids
Synthesized from
arachidonic acid
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What are the sites affected by eicosanoids?
Vascular smooth muscles
Bronchial smooth muscles
Platelets
Cytoprotection (stomach mucus production)
Uterus
(uterine contraction)
Eyes (
intraocular pressure
)
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What is the effect of PGI2 and PGE1?
They cause
vasodilation
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What is the effect of TXA2 and PGF2?
They cause
vasoconstriction
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What is the effect of PGI2 and PGF2alpha?
They cause
bronchodilation
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