Serotonin Drugs Flashcards
5-HT1A agonists
Buspirone
Indications: Generalized Anxiety Disorder,
off label use: w/ SSRI for major depression
MOA: not known, but likely due to activation of post-synaptic
receptors in cortical regions, partial agonist at 5-HT1A receptor
SE: can increase anxiety during initial treatment, drowsiness (but less than benzos),
nausea
Buspirone
5-HT1D receptor Agonists
Sumatriptan
MOA: inhibition of inflammatory mediator
release, cerebrovasconstriction
Indication: Prophylactic for Migraine
SE: Coronary vasoconstriction via 5-HT1D receptor
Contraindication: Pt. with coronary artery disease
Sumatriptan
5HT2C?
Fluoxetine, Sertraline
Indications: depression, PTSD, OCD
MOA: increases 5-HT post-synaptic receptor activation
Takes 2-4 weeks for full effect due to autoreceptor activation
SE: Sexual dysfunction, insomnia
Contraindications: MAO inhibitor, (can cause “serotonin syndrome” )
Fluoxetine, Sertraline
Serotonin antagonist-reuptake inhibitor (SARI)
Trazadone
MOA: 5-HT2A/2C antagonist + SSRI
hypnotic, SSRI, blocks side
effects associated with SSRIs
Indication: Anxiety, Depression (in combination with SSRI)
SE: Warning of suicidality in young adults at initiation of treatment
Contraindication: MAO inhibitors
Trazadone
2nd generation Anti-psychotics
Risperidone
MOA: 5-HT2A /D2/3 antagonist suppresses DA release in mesolimbic pathway, but increases DA release in mesocortical pathway
Indication: Schizophrenia with
Psychosis
SE: weight gain, anxiety, akithesia, psychosis with abrupt discontinuation
Risperidone
5-HT3 receptor antagonist
Ondansetron
Indication: chemotherapy induced emesis
MOA: block 5-HT3 receptor
SE: well tolerated
Ondansetron
5-HT4 receptor agonist
Mosapride (not in US)
Cisapride (discontinued)
See metoclopramide
MOA: 5-HT4 induced stimulation of Ach release in myenteric plexus
Indication: gastroparesis
SE: Arrhythmia (long QT syndrome)
Mosapride (not in US)
Cisapride (discontinued)
See metoclopramide
