Serotonin Flashcards
Lysergic acid diethylamide
Relatively nonspecific - 5HT2 receptors
LSD
Partial or full agonist at 5HT2 receptors
Potency hallucinogen (50 microgram)
Only 1% gets into brain (few nanograms give hallucination)
Buspirone
5-HT1A receptor partial agonist
Antianxiety
Sumatriptan
5 HT 1D and 1B receptor agonists on cerebral blood vessels
Treat migraines and stop existing ones
Inhibit release of vasoactive peptides- calcitonin gene related peptide -CGRP
Promote vasoconstriction
Side effects: nausea, vomiting, angina, dizziness, and flushing
Tegaserod (Zelnorm)
5-HT4 partial agonist Release other enteric NT Normalizes impaired intestinal motility Stimulates intestinal secretion For irritable bowel syndrome with constipation in women Taken off market due to CV effects
Locaserin
Approved for use in treatment of obsesity with adults with BMI greater than 30 or BMI greater than 27 who have at least one weight related health condition like high BP, Type 2 diabetes, high cholesterol
Selective 5-HT 2c receptor agonist–> activation in hypothalamus activates proopiomelanocortin (POMC) production and consequently promote weight loss through satiety
IV drug
Indirect Agonists
SSRI
MOA inhibitors
SNRI
SSRI (Fluoxetine and Duloxetine)
Increase amount of NT in synapse
Treatment: major depressive disorder, OCD, panic attacks
Side effects: sexual dysfunction, nausea
Monoamine oxidase inhibitor
Phenelzine
Block metabolism of serotonin, NE and DA
Increase synaptic serotonin
Treatment of major depressive disorder and narcolepsy
Side effect is food induced hypertensive crisis
SNRI
Duloxetine
Block reuptake of serotonin and NE into neurons
Use: Major depressive disorder and pain
Serotonin Antagonists
Cyproheptadine
Odansetron
Alosetron
Cyproheptadine
5-HT 2 antagonist and H1 histamine antagonist
Treatment for allergies, pruritis and urticaria and carcinoid
Odansetron
5-HT3 antagonists
Treatment of chemotherapy induced nausea and vomiting, post-op and X-Ray therapy induced nausea and vomiting
CNS and GI action
Atypical antipsychotic drugs block 5-HT2 receptors in addition to dopamine receptors
IV, oral and transdermal forms available
Alosetron
Selective 5-HT3 antagonist
Treat diarrhea predominant IBS in women who failed to respond to conventional therapy
Produce severe GI affects like infarcts
Restricted prescribing program
Serotonin Agonists
Lysergic acid diethylamide
Buspirone
Sumatriptan
Duloxetine
Blocks active reuptake of both serotonin and norepinephrine into neurons
Indicated for major depressive disorder and neuropathic pain