Test 2 Seratonin and Dopamine Flashcards
Buspirone
5-HT1a agonist. Likely activates post-synaptic receptors in cortical regions. Partial agonist (but used like a full).
Use: Generalized anxiety disorder. Off-label: w/ SSRI’s for major depression.
Tox: Increased anxiety initial (~2wks), drowsiness, nausea
Sumatriptan
5-HT1d agonist. Inhibition of inflammatory mediator release, cerebro-vasoconstriction.
Use: Prophylactic for migraine
Tox: Coronary vasoconstriction via 5-HT1d receptors
Contra: Coronary artery disease
Fluoxetine
SSRI. Increases 5-HT post-synaptic receptor activation. 2-4weels for full effect from autoreceptor activation.
Use: Depression, PTSD, OCD
Tox: sexual dysfunction, insomnia
Contra: MAO inhibitors (leads to serotonin syndrome (hyperthermia, seizures))
Sertraline
SSRI. Increases 5-HT post-synaptic receptor activation. 2-4weels for full effect from autoreceptor activation.
Use: Depression, PTSD, OCD
Tox: sexual dysfunction, insomnia
Contra: MAO inhibitors (leads to serotonin syndrome (hyperthermia, seizures))
Trazadone
Serotonin antagonist/reuptake inhibitor (SARI) 5-HT2a/c antagonist and SSRI. Blocks SSRI side effects.
Use: Anxiety, depression (with SSRI)
Tox: Suicidality of young adults at treatment initiation
Contra: MAO inhibitors
Risperidone
5-HT2a/D2/D3 antagonist. Decreases dopamine release in mesolimbic pathway, increases dopamine release in mesocortical pathway.
Use: Schizophrenia with psychosis
Tox: Weight gain, akathisia (restlessness), psychosis with abrupt discontinuation
Ondansetron
5-HT3 receptor antagonist.
Use: Chemotherapy-induced emesis (vomiting)
Tox: None, well tolerated
Mosapride
5-HT4 agonist. 5-HT induced simulation of Ach release in myenteric plexus.
Use: Gastroparesis (slowed gut motility)
Tox: Arrhythmia (prolonged QT syndrome)
Not in the US
Cisapride
5-HT4 agonist. 5-HT induced simulation of Ach release in myenteric plexus.
Use: Gastroparesis (slowed gut motility)
Tox: Arrhythmia (prolonged QT syndrome)
Discontinued
L-DOPA
Neurotransmitter precursor. Increases dopamine in nigrostriatal pathway.
Use: Parkinson’s Disease
Tox: Arrhythmia, dyskinesia, (nausea, anxiety, hallucinations, motor fluctuations (long term))
Carbidopa
Amino acid decarboxylase inhibitor. Inhibits L-DOPA conversion to dopamine in the periphery (Carbidopa doesn’t cross BBB).
Use: Concurrent with L-DOPA to decrease its degradation in the periphery
Tox: Augments L-DOPA toxicity.
Bromocriptine
D2 agonist (ergot alkaloid). Postsynaptic activation in basal ganglia, may be neuroprotective (anti-oxidant, free radical scavenger, decreases DNA turnover).
Use: Parkinson’s disease
Tox: (Cardiac valvular fibrosis (long term use), impulse control disorders (rare))
Selegiline
Inhibition of MAO-B (and MAO-A at high doses)
Use: Parkinson’s disease (low dose), depression (higher doses). No dietary tyramine restrictions at lower doses.
Tox: Hypotension (dizziness) low doses, hypertensive crisis (serotonin syndrome) high doses, (dry mouth)
Contra: concomitant use of indirect sympathomimetics or (drugs that increase serotonin transmission)
Tolcapone
Inhibition of COMT. Prolongs/increases effect of L-DOPA, reduces the “off” time, therefore decreasing the amount of L-DOPA needed.
Use: Advanced stage Parkinson’s disease
Tox: (dyskinesia, hallucinations, nausea, hypotension)
Contra: Liver failure (need liver enzyme testing while on the drug)
Haloperidol
D2 antagonist
Use: Acute psychosis, long-term depot for poorly compliant schizophrenic patients
Tox: Extrapyramidal motor disturbances
