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FIU - serotonin receptors
Serotonin receptors
33
Medical
Graduate
12/14/2011

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Term
what type of receptors are 5HT-R?
Definition
all are metabotropic, except 5HT3 - ionotropic
Term
5HT-1A, drug suffix? drug action? use? examples?
Definition
pirone/pidil
agonists
anxiety and hypertension
Buspirone, Urapidil
Term
urapidil
Definition
5HT-1A agonist
also alpha-1 adrenergic antagonist
Term
Buspirone, action? onset? use?
Definition
5HT-1A agonist, moderate D2 affinity, 5HT-2 agonist
onset 4-6 weeks, months for full effect
chronic anxiety
Term
5HT-1D/F, drug suffix? drug action? use?
Definition
triptan
agonists
Migraine - cerebral vasoconstriction and anti-inflammatory
Term
what is the main difference between the various "triptans"?
Definition
t1/2 and metabolism - most by MAO-A, naratriptan by CYP enzymes
Term
what is the most efficacious triptan? administration efficacy?
Definition
sumatriptan
subcutaneous > nasal > oral
Term
triptans are contraindicated in which patients? why?
Definition
cardiovascular disease
they are vasoconstrictors and will increase BP
Term
what drug interactions are possible with triptans? why?
Definition
MAO-I
because triptans are metabolized by MAO-A
Term
MAO-A metabolizes what? MAO-B
Definition
-5HT and NE
-DA
Term
Moclobemide
Definition
MAO-A and B inhibitor - antidepressant
Term
Selegeline
Definition
MAO-A and B inhibitor - anti-Parkinsons
Term
5HT-2, drug action? use?
Definition
antagonist
psychosis
Term
Pizotifen
Definition
5HT-2 antagonist and H1 antagonist
migraines
Term
Mianserin
Definition
5HT-2 antagonist
anxiety and depression
Term
Ritanserin
Definition
5HT-2 antagonist
anxiety and depression
Term
ketanserin
Definition
5HT2 antagonist and alpha1-blocker
hypertension, Raynaud's (spasm of femoral artery)
Term
nefazadone
Definition
5HT2 antagonist and SSRI
antidepressant
off market - liver damage
Term
trazodone
Definition
5HT2 and SSRI
antidepressent
still on market
Term
Quetieapine
Definition
5HT2 antagonist and D2 blocker (equally)
antipsychotic
Term
olanzepine
Definition
5HT2 antagonist > D2 blocker
antipsychotic
Term
Ziprasidone
Definition
5HT2 antagonist >>> D2 blocker
antipsychotic
Term
Aripiprazole
Definition
5HT2 antagonist and 5HT-1A agonist
antipsychotic
no weight gain or risk of torsades
Term
5HT3, drug suffix, drug action, use
Definition
setrons
antagonist
anti-emesis, diarrhea, IBS
Term
Palanosetron
Definition
5HT3 antagonist
extremely long acting
given i.v. once before each cycle of chemotherapy
Term
5HT-4, drug suffix, drug action, use
Definition
pride
agonist (increase ACh)
gastroparesis
Term
metoclopramide; action, use, SEs
Definition
5HT-4 agonist, D2 agonist, 5HT-3 antagonist, cholinesterase inhibitor
anti-nausea and vomiting
tarditive dyskinesia
Term
cisapride
Definition
5HT-4 agonist
off market - interfered with K-channel blockers -> torsades
Term
mesapride
Definition
5HT-4 agonist
essentially cisapride w/o K-blockage
Term
SEs of SSRIs
Definition
delayed ejaculation and hyperthermia
Term
which SSRIs don't inhibit CYP P450 enzymes
Definition
citalopram and sertraline
Term
what is the most popular SSRI? why?
Definition
citalopram, it is the most selective for 5HT, and has minimal P450 inhibition
Term
Venlafaxin
Definition
essentially a tricyclic antidepressant without the SEs
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