Antidepressants Flashcards by Shiv Krishnan

What form of drugs best crosses the BBB?

lipophilic/hydrophobic

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Name 4 classes of Monoamine Reuptake Inhibitors?

tricyclics
SSRIs
NA reuptake inhibitors
other non-selective reuptake inhibitors

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What do Monoamine Transmitters contain structurally?

-a single AMINE (NH2) group

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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

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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

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What is the Caudal- Raphe nuclei responsible for?

Analgesia

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What is the Rostral Raphe nuclei said to regulate?

sleep
mood
feeding
sensory perception

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What enzyme converts 5-OH-Tryptophan to 5-HT?

L-AA Decarboxylase

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What metabolized 5-HT?

-Monoamine Oxidase

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Where is the Main site of noradrenaline neurones in the brain?

Locus Caeruleus

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What is the major REGULATORY role of Locus CAERULEUS?

regulation of arousal, attention and stress response

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Name 2 monoamine oxidase inhibitors.

Phenelzine

- Moclobemide

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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

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What is the risk of using Irreversible MAO-Is? (1)

“CHEESE REACTION” may occur (a hypertensive crisis)

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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

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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

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What other S/Es do MOA-Is bring about?

insomnia
postural HYPOTENSION
peripheral edema
potentiates other drugs (benzos) by decreasing their metabolism

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Where is tyramine found?

in cheese
yeast containing products (beer, wine, sauces)
old food

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Which irreversible Monoamine Oxidase Inhibitor must one carefully monitor their diet for?

Phenelzine

Name 3 tricyclic Antidepressants.

imi- and Lofe-pramine
amitriptyline
dosulepin

How do Tricyclic antidepressants act?

blocks the reuptake of MONOAMINES (NE and 5-HT) into the presynaptic terminals

What are the COMMON s/es of TCAs?

- Anticholinergic S/Es: 
blurry vision, dry mouth, constipation, urinary retention
-SEDATION, WGT GAIN
- tachycardia, Arrhythmia
- HYpotension

Why should TCAs not be considered for cardiac patients?

cardiotoxic
postural hypotension
tachycardia
arrhythmias

Name a SSRI and its mode of axn.

FLUOXETINE

- block the serotonin reuptake transporter

Name 3 other SSRIs.

- citalopram - sertraline - Paroxetine

What are the s/es of SSRIs?

- Nausea - Headache - Sweating - Anxiety worsened - WGT gain, sedation - sexual DYSFXN - hyponatremia (in the old)

Which age group of individuals should you be wary about with SSRIs?

- pts < 25Y.O | - risk of SELF-HARM and suicidal ideation

Why are there a no. of GI s/es with use of SSRIs?

- d/t stimulation of serotonin receptors in the GIT

Name 2 DUAL reuptake inhibitors.

- Venlafaxine - Duloxetine - both blocks NE and 5-HT

Why are dual reuptake inhibitors preferred?

- d/t their LACK of major receptor blocking axns

Name an atypical antidepressant and what receptors it blocks.

Mirtazapine | blocks alpha2, 5-HT2 and 5-HT3

What are the s/es of Mirtazapine?

incr. appetite>WGT gain and confusion

which other anti-depressants may be given adjunct to SSRIs to reduce its s/es?

mirtazapine - because it blocks post-synaptic serotonin receptors; highly serotonergic

Name a dopamine uptake inhibitor.

Bupropion

How efficient are anti-depressants, in general?

- all of them: 40-70% efficacy - most: delayed ONSET of action - BEST used for only SEVERE depression

What is the MOA of Lithium?

- said to block the second messnger sys. / inhibit GLYCOGEN SYNTHASE KINASE 3BETA

What is a sign that blood level of Lithium is very high?

- ATAXIA - vomitting - diarrhea - convulsions - coma

Other s/es of Lithium?

- dry mouth - polydipsia/polyuria - hypothyroidism - tremor - long term reduced renal function - wgt gain - NEPHROGENIC diabetes insipidus

What is given as long term treatment as Mood Stabilizers?

- Valproic Acid, Lamotigrine, Carbamazepine (ANTICONVULSANTS)

What MAJOR risk does Valproic Acid hold?

teratogenecity ---others: ataxia, drowsiness, liver enzyme induction (shared with CARBAMAZEPINE)

What risk does lamotigrine hold?

small risk of STEVEN-JOHNSON $

What is lithium used for?

- as a mood stabilizer in Bipolar d/o

What anti-psychotics can be given as a mood stabilizer?

- olanzapine - quetiapine - lurasidone - Aripiprazole

What is the MOA of anti-psychotic?

-dopamine antagonist and serotonin antagonist

What are the S/Es of antipsychotics?

sedation, wgt gain, METABOLIC SYNDROME | - extrapyramidal effects (aripiprazole)

What to give an obese pt who has come in with depression?

- avoid: Mirtazapine, TCA, Lithium, Atypical Anti-psychotic GIVE VENLAFAXINE, BUPROPION