Antidepressants Flashcards
What form of drugs best crosses the BBB?
- lipophilic/hydrophobic
Name 4 classes of Monoamine Reuptake Inhibitors?
- tricyclics
- SSRIs
- NA reuptake inhibitors
- other non-selective reuptake inhibitors
What do Monoamine Transmitters contain structurally?
-a single AMINE (NH2) group
What is the relation between Monoamine NT and Depression?
- one of the many reasons depression occurs is d/t the DEFICIT of M-NT; esp. 5-HT and NA
- why CSF of depressed patients contain REDUCED Monoamine levels
What are Raphe Nuclei?
- nuclei found running down from the brain stem to the spinal cord
- 2 groups- caudal and rostral
- said location for SEROTONIN prodn
What is the Caudal- Raphe nuclei responsible for?
- Analgesia
What is the Rostral Raphe nuclei said to regulate?
- sleep
- mood
- feeding
- sensory perception
What enzyme converts 5-OH-Tryptophan to 5-HT?
L-AA Decarboxylase
What metabolized 5-HT?
-Monoamine Oxidase
Where is the Main site of noradrenaline neurones in the brain?
- Locus Caeruleus
What is the major REGULATORY role of Locus CAERULEUS?
- regulation of arousal, attention and stress response
Name 2 monoamine oxidase inhibitors.
- Phenelzine
- Moclobemide
How do MOA-Is help increase NT levels?
- less NT is metabolized in the post-synaptic neurone
- less NT will be re-uptaken
- More NT remains in the synaptic cleft==>more activity
What is the risk of using Irreversible MAO-Is? (1)
- “CHEESE REACTION” may occur (a hypertensive crisis)
How does the cheese reaction come about?
- irreversible MAO-Is permanently deactivates MAO; it would then take a couple of weeks for the enzyme levels to be restored
- therefore essential to control tyramine intake
How does Tyramine levels cause malignant hypertension?
- tyramine is a potent releaser of NE.
- with the use of MAO-Is and intake of tyramine; NE levels will surge ==> ^BP
What other S/Es do MOA-Is bring about?
- insomnia
- postural HYPOTENSION
- peripheral edema
- potentiates other drugs (benzos) by decreasing their metabolism
Where is tyramine found?
- in cheese
- yeast containing products (beer, wine, sauces)
- old food