SEROTONIN (autacoids)

serotonin is aka ___________________

5-hydroxytryptamine (5-HT)

serotonin is produced by ______________ [__%], _____ and ______

enterochromaffin (ECF) cells [>90%]
platelets,
and CNS

name the precursor of serotonin (5HT)

tryptophan (W)

name the serotonin (5HT) receptor/s with the effect:
inhibition of release of serotonin

5-HT1A

name the serotonin (5HT) receptor/s located in:

CNS

5-HT1A

name the serotonin (5HT) receptor/s with the effect:
vasoconstriction (anti-migraine)

5-HT1B/1D

name the serotonin (5HT) receptor/s located in:

cerebral blood vessels

5-HT1B/1D

name the serotonin (5HT) receptor/s with the effect:

contraction
- vasoconstriction
- oxytosis
- bronchoconstriction

5-HT2A/2B

name the serotonin (5HT) receptor/s located in:

smooth muscles
- blood vessels
- uterus
- bronchi

5-HT2A/2B

name the serotonin (5HT) receptor/s with the effect:

proaggregation

5-HT2A/2B

name the serotonin (5HT) receptor/s located in:

platelets

5-HT2A/2B

name the serotonin (5HT) receptor/s with the effect:
vomiting (emesis)

5-HT3

name the serotonin (5HT) receptor/s located in:

chemoreceptor trigger zone (CTZ)

5-HT3

name the serotonin (5HT) receptor/s with the effect:
peristalsis

5-HT4

name the serotonin (5HT) receptor/s located in:

gastrointestinal tract (GIT)

5-HT4

this is known as one of the safest drugs for anxiety, due to its lesser risks for dependence, addiction, and potential abuse for the drug.

buspirone

a 5-HT1A PARTIAL AGONIST that is an anxiolytic

buspirone

buspirone is a 5-HT__________ (AGONIST / ANTAGONIST)

5-HT1A partial agonist

these are 5-HT1B/1D agonists that are the DOC for acute migraine

-triptans

name all the “-triptan” drugs

sumatriptan (Imigran)
naratriptan
zolmitriptan

a drug that is a 5-HT1B/1D agonist that is not taken ORALLY, but intranasally, transdermally, IV

sumatriptan (Imigran)

“-triptan” drugs are 5-HT________ (ANTAGONISTS / AGONISTS)

5-HT1B/1D AGONISTS

_________ derivatives are 5-HT2A/2B AGONISTS

ergot derivatives

ergot derivatives are 5-HT ____________ (ANTAGONISTS / AGONISTS)

5-HT2A/2B AGONISTS

an ergot derivative drug that is used as treatment for migraine

ergotamine

an ergot derivative drug that is vasoselective

ergotamine

ergotamine is (UTERO / VASO)selective

vasoselective

are ergot derivatives that induces uterine contraction

ergonovine, ergometrine

are ergot derivatives that are used in the management of postpartum bleeding

ergonovine, ergometrine

ergot derivatives that are uteroselective

ergonovine, ergometrine

ergonovine, ergometrine are (UTERO / VASO)selective

uteroselective

give adverse effects/toxicities of ergot derivatives:

_______________
_______________
_______________

hypertension
oxytoxic
retroperitoneal fibrosis

a 5-HT2A/2B Antagonist that is used as prophylaxis for migraine

methylsergide

a 5-HT2A/2B Antagonist that is used as an anti-hypertensive drug

ketanserine

methylsergide is a 5-HT____ (ANTAGONIST / AGONIST)

5-HT2A/2B ANTAGONIST

ketanserine is a 5-HT____ (ANTAGONIST / AGONIST)

5-HT2A/2B ANTAGONIST

the most common toxic effect of 5-HT2A/2B ANTAGONISTS

GI disturbances

the most serious toxic effect of 5-HT2A/2B ANTAGONISTS

gangrene

the unique toxic effect of 5-HT2A/2B ANTAGONISTS

retroperitoneal fibrosis

a 5-HT1/2 Antagonist that is used for treatment of serotonin syndrome

cyproheptadine

cyproheptadine is a 5-HT____________ (ANTAGONIST / AGONIST)

5-HT1 and 2 ANTAGONIST

give symptoms of serotonin syndrome: (STAGE)
______________________
______________________
______________________
______________________
______________________

shivering & sweating
tachycardia & hypertension
agitation & altered mental status
GI upset (diarrhea, nausea)
exaggerated reflexes (hyperreflexia, clonus)

“-setrons” drugs are 5-HT____ (ANTAGONISTS / AGONISTS)

5-HT3 ANTAGONISTS

are 5-HT3 antagonists that are used for the management for chemotherapy-induced nausea and vomiting (N&V)

-setrons

name “-setrons” drugs: APOG

alosetron
palonosetron
ondansetron
granisetron

a 5-HT3 antagonist that is used for treatment of irritable bowel disease (IBD)

alosetron

5-HT______ Agonists are used for treatment for irritable bowel syndrome

5-HT4

name drugs under 5-HT4 PARTIAL AGONISTS:

cisapride
tegaserod

cisapride and tegaserod are 5-HT4 (PARTIAL / FULL) agonists

partial

name drugs under 5-HT4 FULL AGONISTS:

prucalopride

prucalopride is a 5-HT4 (PARTIAL / FULL) agonist

full agonist