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CNS 2 Spears

Depression and Antidepressants

QuestionAnswer
What are the types of depression? MDD--> Persistent Depressive Disorder Anxious Depression Atypical Depression Melancholic Depression Mood reactivity + Hypersomnia/Increased appetite & weight -Psychotic depression -Peripartum/postpartum depression -Tx resistant depression
Peripartum/Postpartum depression (PPD) has 2 medications available, which are? *not the baby blues (difference due to persistence of depression symptoms) 1) Zuranolone oral treatment for PPD (approved 2023) GABA-A modulator, mimic allopregnanolone 2) Brexanolone I.V. treatment for PPD (approved 2019) MOA: positive GABA-A receptor modulator Boxed warning  excessive sedation, sudden loss of consciousness
MDD (Major depressive disorder) definition? Persistent, low mood with loss of enjoyment and pleasure
Causes of depression can be? Genetic, environmental, psychological, Biochemical (NT, Inflammatory markers)
Differences b/w monoamines--> Which of the monoamines are classified as Catecholamines? DA and NE
Differences b/w monoamines--> Which of the monoamines is not considered a catecholamine? Serotonin
What is the precursor of dopamine? Tyrosine
Precursor of NE? Tyrosine
Precursor to Serotonin? Tryptophan
The _____ system is known as the emotional brain Limbic -brain stem, amygdala, hippocampus, hypothalamus
What area of the brain is known as the cognitive brain? prefrontal cortex
depression is caused by a ______ in monamines (5-HT, DA, NE) decrease *depression + tx = increase in monoamines
What are the names of the 2 hypothesis? 1. Monoamine hypothesis 2. Neurotropic hypothesis
The monoamine hypothesis is? Deficency in the amount or function of 5-HT, NE, or DA
Monoamine hypothesis: *NTs are differently _______ in depression subtypes imbalanced *not necessarily a deficency that the body is not making it at all, but in certain brain regions and in certain symptoms of depression, some are more active or less active than others. This could be incorporated (not only in decreases in the production of the NT byt also the effectiveness at its receptor
I.e. Atypical depression: may not benefit from a medication that prefers to increase 5-HT, might need a medication that has a bigger effect on ________ Noradrenegic and DA increasing
Melancholic depression has more Noradrenergic and 5-HT and less ______ DA
T/F the monoamine hypothesis and the neurotropic hypothesis happen at different times False (they occur at the same time)
What is the Neurotropic (Stress) hypothesis? there is a decrease in brain-derived neurotrophic factor (BDNF) -BDNF promotes synaptic remodeling (i.e an incerase in dendrict sprouts--> and when there is more dendritic sproites, there are more synapes so the NT can be more effective but with this hyptheis there is less BDNF
What is the reasons antidepressants take a long time to work? in the body, the amount of NT's increase rapidly at the synapse so the reason these medications take a long time to work isnt b/c of how long it takes to generate more NT's its bc it takes a long time (3-8 wks to increase BDNF so that there is more expression of dendritic sprouts
In a treated state as shown in the Neurotrophic hypothesis--> BDNF is elevated to get more dendritic sprouts. More sprouts menas more synapses, menaing more of that neuronal connections that can be occuring--> more effectveness of tht NT that are released from those areas
what drug classes are transport blockers? SSRIs; SNRIs; TCAs; NDRI
What class of drug is a degradation blocker? MAOIs
________ antidepressants are classified as "other" atypical
general SE of blocking adrenergic a-1 receptors? orthostatic hypotension
general SE of blocking Histamine (H1) receptors? Drowsiness and weight gain
general SE of blocking cholinergic, mACh, M1 receptors? ANTI-SLUDGE (dry mouth, constipation, confusion)
general SE of receptor activation of Serotonin, 5H2 receptors? Sexual dysfunction -Serotonin is centrally and peripherally acting
general SE of activating 5HT2 receptors? insomnia/agitation
general SE of activating 5HT3 receptors? GI/Nausea
general SE of activating NE receptors? hypertension/increased HR
When using meds that activate the receptor, do we want high or low doses? LOW
______ syndrome is true for ALL antidepressants Discontinuation -Unmonitored tapering/end  abrupt changes in brain Dizziness, nausea, anxiety, agitation, lethargy Shorter half-life = More of a problem (e.g., paroxetine)**
Which antidepressant has a shorter 1/2 life so that discontinuation syndrome is more of a problem? Paroxetine
What is serotonin syndrome toxicity? Mild to severe neuromuscular & autonomic hyperactivity
Suicide risk (ideation attemps are _____ for ALL antidepressants TRUE *greater risk in younger ages *immediate notifications
Which medications are classified as SSRIs? Citalopram (Celexa ®) & Escitalopram (Lexapro®) Fluoxetine (Prozac®) Fluvoxamine (Luvox®) (*also for OCD) Paroxetine (Paxil®) Sertraline (Zoloft®)
_____ has a higher risk of sexual dysfunctio, weight gain, and discontinuation syndrome Paroxetine
Which SSRI has the longest 1/2 life? Fluoxetine
Which SSRI has the shortest 1/2 life? Paroxetine
This SSRI has activitity not only on SERT but can also has antagonist activation at NET, M1, and a1? Paroxetine
Fluoxetine has antagonist activity not only at SERT but also on? 5-HT2
Vortioxetine (Trintellix) is an SSRI with antagonism at SERT and also on ____ NET Agonist: 5-HT1A Partial agonist: 5-HT1B Antagonist: 5-HT1D, 5-HT3, 5-HT7
Which drugs are SNRIs? Venlafaxine (Effexor®) & Desvenlafaxine (Pristiq®) Duloxetine (Cymbalta®) Milnacipran (Savella®) & Levomilnacipran (Fetzima®)
SE of SNRIs include? Sexual dysfunction Nausea Headache, dizziness Sedation Insomnia Increased blood pressure, hr **Discontinuation & Serotonin Syndromes**
SNRIS such as _______ have less antagonist activity at the off-target receptors (5-HT2, H1, M1, a1) Venlafaxine/Desvenlafaxine Duloxetine Milnacipran/Levomilnacipran
Duloxetine has ____ affinity for atagonist acitivty at SERT and NET equal (+++)
Venlafaxine/Desvenlafaxine have ++ at the ______ and + at _____ SERT; NET
Milnacipran/Levomilnacipran have + at the _____ and +++ at ___ SERT; NET *favors NET
TCA medications include? Amoxapine Amitriptyline (Elavil®) Nortriptyline (Pamelor®) Doxepin (Sinequan®) Imipramine (Tofranil®) Clomipramine (Anafranil®) Desipramine (Norpramin®)
TCA MOA? SERT & NET Blockers + Non-specific receptor blockers
TCA class Notes? (4) -Narrow TI -Cardica Toxicity (Na+ channel blockers) -Seizures -Discontinuation syndrome
The following TCAs are classified as secondary amines: Amoxapine; Nortriptyline (Pamelor); Desiprmaine (Norprmain)
The following TCAs are classified as tertiary amines: amitriptyline; doxepin; imipramine; clomipramine
TCAs cause lots of ADRs (T/F) True (ton of off-target receptor binding so more AE compared to traditional exclusive blockers)
What AE are caused by anti-histaminergic? sedation, increased appetite
What AE are caused by Anti-muscarinic? Anti-SLUD effects: dry mouth, urinary retention, constipation + confusion, arrythmias
What AE are caused by Adrenergic a1? Orthostatic hypotension
TCA MOA is? blocks 5-HT, NET, H1, and muscarinic receptors
NDRI (Norepinephrine and Dopamine Reuptake Inhibitor drug is? Bupropion (Wellbutrin, Zyban)
MOA of Bupropion: DAT(>>>) & NET Blocker Presynaptic NT release *favors DAT
AE of Bupropion includes? -Insomnia - Seizures - Hypertension - Hallucinations/Psychosis
CI of Bupropion? -Antiepileptic drugs -Eating disorders -MAOIs
Bupropion comes with low risk of? Sexual dysfunction (due to bupropion not targeting serotonin), nausea (b/c its not hitting 5-HT3), weight gain (not hitting the H1 receptor)
Which medications are classified as MAOIs? Phenelzine (Nardil®) Isocarboxazid (Marplan®) Selegiline (patch) – (Emsam®) Tranylcypromine (Parnate®) PIST
MOA for MAOIs? inhibit MAO causing monoamines to not get broken down so there will be an increase in NTs available in the sybaptic space and in the cleft
where do MAOIs work? centrally and peripherally
Lifespan of MAOIs? 2-3 weeks
MAOIs are irreversible and ______ non-selective
Created by: Xander635
Popular Pharmacology sets

 

 



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