Dopamine and Serotonin Flashcards
Sumatriptan target and function
5‐HT1D receptor Agonist - treats migraines
Inhibition of inflammatory mediator release Cerebrovasconstriction
Sumatriptan indication
Migraines
Sumatriptan toxicity
Coronary vasoconstriction
Sumatriptan contraindication
Coronary artery disease
How is the 5-HT1D family of receptors is manipulated to treat migraine?
5-HT1D agonists like sumatriptan inhibits inflammatory mediator release with cerebral vasoconstriction
How are 5-HT1A receptors manipulated pharmacologically for treatment of anxiety and depression?
5-HT1A agonists like buspirone lead to the activation of post‐synaptic receptors in cortical regions
How are 5-HT3 receptors manipulated pharmacologically for the treatment of chemotherapy-induced nausea and emesis?
There are 5-HT3 antagonists like ondansetron that reduce cancer treatment related emesis
How is the 5-HT4 receptor manipulated for treatment of GI disorders?
5-HT4 agonists like mosapride will stimulate ACh release in the myenteric plexus which treats things like gastroparesis
Buspirone target and function
5-HT1A partial agonist
Activation of post‐synaptic receptors in cortical regions
Buspirone indication
Anxiety
Depression
Buspirone toxicity
Early increase in anxiety
5-HTP function
5-HT precursor
5-HTP indication
Depression
Risperidone target and function
5-HT2A/2C antagonist and D2/3 antagonist
Suppresses DA release in mesolimbic pathway, but
increases DA release in mesocortical pathway.
Increased activity in mesolimbic causes hallucinations
Decreased activity in mesocortical causes poor emotional affect
Risperidone indication
Schizophrenia with psychosis
Risperidone toxicity
Weight gain
Akithisia - restlessness
Ondasetron target and function
5-HT3 antagonist
Reduces emesis
Ondasetron indication
Chemotherapy induced emesis
Ondasetron toxicity
None. Well tolerated in patients.
Fluoxetine/Sertraline target and function
SSRI
Increases 5-HT (serotonin) post-synaptic receptor activation
Fluoxetine/Sertraline indication
Depression OCD Anxiety Panic disorder PTSD Social phobia
Fluoxetine/Sertraline toxicity
Sexual dysfunction
Insomnia
Fluoxetine/Sertraline contraindications
MAO inhibitors as it can cause “serotonin syndrome”
L-DOPA effect
DOPA precursor
L-DOPA indication
Parkinson’s Disease
L-DOPA toxicity
Arrhythmia
Dyskinesia
Carbidopa effect
Inhibits AADC in peripheral tissue but cannot cross BBB.
Used with L-DOPA to minimize peripheral DOPA
Carbidopa indication
Concurrent rx with L‐DOPA to reduce peripheral DA production to protect the CV system
Carbidopa toxicity
Augments SE of L‐DOPA in CNS
Selegiline target and effect
MAO-B inhibitor to increase DOPA
Selegiline indication
Low dose: Parkinson’s Disease
High dose: Depression
Selegiline toxicity
Potential for hypertensive crisis
Bromocriptine target and effect
D2 agonist
Post synaptic activation in basal ganglia, may also be neuroprotective so best used early in disease. Leads to increased DOPA
Bromocriptine indication
Parkinson’s Disease
Bromocriptine toxicity
Arrhythmia
Dyskinesia
Tolcapone target and effect
Inhibits COMT breakdown of DOPA
Tolcapone indication
Parkinson’s Disease
Tolcapone toxicity
Prolongs and increases effect of L‐DOPA, reduces “off” time, can reduce required L‐DOPA dose
Tolcapone contraindication
Liver failure
Haloperidol target and effect
D2 antagonist
Haloperidol indication
Psychosis
Haloperidol toxicity
Extra- pyramidal motor disturbances
Methylphenidate target and effect
Increased DA release in frontal cortex
Methylphenidate indication
ADHD
Methylphenidate toxicity
Tachycardia
Methylphenidate contraindication
Tricyclic antidepressants
Metaclopramide target and effect
D2 antagonist
Metaclopramide indication
Chemotherapy‐induced‐ and post‐op nausea and vomiting
Metaclopramide toxicity
Akathisia
Metaclopramide contraindication
Long term prescription
Trazadone target and effect
5‐HT2A/2C antagonist + SSRI
Trazadone indication
Anxiety
Depression
Trazadone toxicity/contraindication
Warning of suicidality in young adults at initiation of treatment
Contraindication: MAO inhibitors
Mosapride/Cisapride target and effect
5‐HT4 receptor agonist
Promotes GI motility
Mosapride/Cisapride indication
Gastroparesis
Mosapride/Cisapride toxicity
Prolonged QT syndrom