Antidepressants Flashcards
Clomipramine
MOA?
- Mainly inhibits 5HT reuptake
Sertraline MOA class
Fewer interactions than?
- SSRI
- less 2D6 so less interactions
Bath salts
MOA
4 x more potent as a stimulant than ritalin
- NE and dopamine reuptake inhibitor
Paroxetine
MOA
What about toxicity?
- SSRI
- methylenedioxy ring—> more toxic
- Michael acceptor
- Quinone formation from methylene
Nefazodone
Class
MOA
Less sedation than?
- Phenylpiperazine
- 5HT uptake inhibition
- Some NE uptake inhibition
- 5HT2 antagonist
- Less sedation compared to TCAs and Trazodone
Imipramine
MOA
Prototype
Class
Causes more what in comparison to other drugs in this class?
Metabolism
Presence of tertiary nitrogen gives it more?
- TCA
- inhibits reuptake of S > NE
- more orthostatic hypotension than amitriptyline
- Dealkylation will give active metabolites
- Tertiary > Anticholinergic SEs, But less than amitriptyline
Fluoxetine
MOA
Metabolism
Dont use with?
- SSRI
- 2D6
- Dont use with TCAs or MAOIs
Citalopram
MOA
What needs to be watched?
Escitalopram
- SSRI
- QT prolongation
- Escitalopram is the S-enantiomer less prolongation
Nisoxetine
MOA
Class
- SNRI
- Contains chiral center
What are the advantages and AEs of SSRIs
- Less cardiavascular toxicity than TCAs
- Less sedation
- Lower toxicity in OD compared to MAOIs and TCAs
- AEs: Anxiety, sexaul dysfunction, nausea
SAR for TCAs
- Amine substitution
- _ carbons between tricyclic ring and amine
- _____ on tricyclic ring increses affinity for?
- Tertiary
- S reuptake > NE reuptake
- More orthostatic hypotension than secondary
- Generally more anticholinergic SEs
- Secondary
- NE reuptake > S
- less sedation compared to tertiaty
- 3 carbons between tricyclic ring system and amine
- Halogen on tricyclic system increases affinity for 5-HT transporter
Trancypramine
MOA
Prototype Structure
What is the irreversible portion of this drug?
Since this is irreversible what is more likely to take place?
- Irreversible MAO- Inhibitor
- Triangle banana bond give it the irreversible nature
- More likely to have toxic effects due to the covalent bond that is formed
Amitriptyline
MOA?
Whats the difference with this one compared to others in this class?
R=CH3
- S>NE
- TCA
- Does not contain a Nitrogen in ring instead has a C=C these have the same geometry though so they can be interchanged but steriochemistry becomes important
Moclobemide
MOA?
Has less?
- Reversible MAO-A Inhibitor
- Less toxic effects compared to irreversible
Venlafaxine
MOA
what SEs are low?
R=CH3
- NE/S reuptake inhibitor
- Low anticholinergic, sedation, and orthostatic hypo
Bupropion
Class
MOA
Looks like?
Minimal what SE?
- Phenylethylamines
- Weak dopamine uptake inhibitor
- Very weak NE and S uptake inhibitor
- Looks like amphetamine so the dopamine part makes sense
- Less Sexual AEs
Amoxapine
R=H
MOA
Similar to?
Antagonist at what receptors?
Class?
Metabolite of?
- EPS
- TCA
- 51C - 2 and 3
- Similar to desipramine
- Metabolite of Loxapine
Mirtazepine
MOA
Class
Antagonism where else?
- NE/S reuptake inhibitor
- a1 and H1 antagonist
- 5HT2 and 3 not 1
Trimipramine
MOA?
- Inhibits reuptake of both NE and S
- Alkylation on the 3 carbon provides less anticholinergic SEs
Vilazodone
MOA
- Agonist at 5 HT 1A partial
- SSRI
Protriptyline
Isomer of nortriptyline
MOA?
Class
Contains what? Possible?
- TCA
- NE more
- C=C possible epoxidation
Duloxetine
MOA
What else can this be used to treat?
- SNRI
- Can be used to treat:
- Diabetic Nueropathy
- pain control in fibromyalgia
- Chronic musculoskeletal pain
Doxepin
MOA?
Only used?
Class?
- TCA
- NE and S
- Used topically as H1 antagonist
Reboxetine
MOA
- SNRI
Selegiline
MOA?
- Irreversible non selective MAO I
Desipramine
R=H
MOA?
Activity at?
- TCA
- Activity more at NE
Nortriptyline
R=H
MOA
Class
- TCA
- S and NE equally
Vortioxetine
MOA
whats special about it?
- SSRI
- active at many receptors
- antagonist at: HT1D, HT3, HT7
- Steric hinderance of ring decreases rate of metabolism
EsKetamine
MOA
This has been known to ____ compared to SSRIs or SNRIs
- NMDA antagonist
- Known to be faster acting compared to SSRIs and SNRIs this can be benficial because they take so long to take effect
Phenelzine
What group is present?
MOA?
- Irreversible non-selective MAO I
- Hydrazine group present
In general TCAs what is the difference betwen secondary and tertiary nitrogens?
- Tertiary S > NE
- Secondary NE > S
Isocarboxazid
MOA?
- Irreversible MAO I
Trazodone
MOA
what gives it the Serotonin activity?
Class?
- phenylpiperazine
- 5HT uptake inhibitor
- 5HT2A antagonist
- Sedation
- Piperazine with phenyl CL gives serotonin activity
