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Medicinal Chem > Antidepressants > Flashcards

Antidepressants Flashcards

1
Q

Clomipramine

MOA?

A
  • Mainly inhibits 5HT reuptake
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2
Q

Sertraline MOA class

Fewer interactions than?

A
  • SSRI
  • less 2D6 so less interactions
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3
Q

Bath salts

MOA

4 x more potent as a stimulant than ritalin

A
  • NE and dopamine reuptake inhibitor
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4
Q

Paroxetine

MOA

What about toxicity?

A
  • SSRI
  • methylenedioxy ring—> more toxic
  • Michael acceptor
  • Quinone formation from methylene
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5
Q

Nefazodone

Class

MOA

Less sedation than?

A
  • Phenylpiperazine
  • 5HT uptake inhibition
    • Some NE uptake inhibition
  • 5HT2 antagonist
  • Less sedation compared to TCAs and Trazodone
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6
Q

Imipramine

MOA

Prototype

Class

Causes more what in comparison to other drugs in this class?

Metabolism

Presence of tertiary nitrogen gives it more?

A
  • TCA
  • inhibits reuptake of S > NE
  • more orthostatic hypotension than amitriptyline
  • Dealkylation will give active metabolites
  • Tertiary > Anticholinergic SEs, But less than amitriptyline
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7
Q

Fluoxetine

MOA

Metabolism

Dont use with?

A
  • SSRI
  • 2D6
  • Dont use with TCAs or MAOIs
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8
Q

Citalopram

MOA

What needs to be watched?

Escitalopram

A
  • SSRI
  • QT prolongation
  • Escitalopram is the S-enantiomer less prolongation
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9
Q

Nisoxetine

MOA

Class

A
  • SNRI
  • Contains chiral center
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10
Q

What are the advantages and AEs of SSRIs

A
  • Less cardiavascular toxicity than TCAs
  • Less sedation
  • Lower toxicity in OD compared to MAOIs and TCAs
  • AEs: Anxiety, sexaul dysfunction, nausea
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11
Q

SAR for TCAs

  1. Amine substitution
  2. _ carbons between tricyclic ring and amine
  3. _____ on tricyclic ring increses affinity for?
A
  • 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
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12
Q

Trancypramine

MOA

Prototype Structure

What is the irreversible portion of this drug?

Since this is irreversible what is more likely to take place?

A
  • 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
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13
Q

Amitriptyline

MOA?

Whats the difference with this one compared to others in this class?

R=CH3

A
  • 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
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14
Q

Moclobemide

MOA?

Has less?

A
  • Reversible MAO-A Inhibitor
  • Less toxic effects compared to irreversible
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15
Q

Venlafaxine

MOA

what SEs are low?

R=CH3

A
  • NE/S reuptake inhibitor
  • Low anticholinergic, sedation, and orthostatic hypo
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16
Q

Bupropion

Class

MOA

Looks like?

Minimal what SE?

A
  • Phenylethylamines
  • Weak dopamine uptake inhibitor
  • Very weak NE and S uptake inhibitor
  • Looks like amphetamine so the dopamine part makes sense
  • Less Sexual AEs
17
Q

Amoxapine

R=H

MOA

Similar to?

Antagonist at what receptors?

Class?

Metabolite of?

A
  • EPS
  • TCA
  • 51C - 2 and 3
  • Similar to desipramine
  • Metabolite of Loxapine
18
Q

Mirtazepine

MOA

Class

Antagonism where else?

A
  • NE/S reuptake inhibitor
  • a1 and H1 antagonist
  • 5HT2 and 3 not 1
19
Q

Trimipramine

MOA?

A
  • Inhibits reuptake of both NE and S
  • Alkylation on the 3 carbon provides less anticholinergic SEs
20
Q

Vilazodone

MOA

A
  • Agonist at 5 HT 1A partial
  • SSRI
21
Q

Protriptyline

Isomer of nortriptyline

MOA?

Class

Contains what? Possible?

A
  • TCA
  • NE more
  • C=C possible epoxidation
22
Q

Duloxetine

MOA

What else can this be used to treat?

A
  • SNRI
  • Can be used to treat:
    • Diabetic Nueropathy
    • pain control in fibromyalgia
    • Chronic musculoskeletal pain
23
Q

Doxepin

MOA?

Only used?

Class?

A
  • TCA
  • NE and S
  • Used topically as H1 antagonist
24
Q

Reboxetine

MOA

A
  • SNRI
25
Q

Selegiline

MOA?

A
  • Irreversible non selective MAO I
26
Q

Desipramine

R=H

MOA?

Activity at?

A
  • TCA
  • Activity more at NE
27
Q

Nortriptyline

R=H

MOA

Class

A
  • TCA
  • S and NE equally
28
Q

Vortioxetine

MOA

whats special about it?

A
  • SSRI
  • active at many receptors
  • antagonist at: HT1D, HT3, HT7
  • Steric hinderance of ring decreases rate of metabolism
29
Q

EsKetamine

MOA

This has been known to ____ compared to SSRIs or SNRIs

A
  • NMDA antagonist
  • Known to be faster acting compared to SSRIs and SNRIs this can be benficial because they take so long to take effect
30
Q

Phenelzine

What group is present?

MOA?

A
  • Irreversible non-selective MAO I
  • Hydrazine group present
31
Q

In general TCAs what is the difference betwen secondary and tertiary nitrogens?

A
  • Tertiary S > NE
  • Secondary NE > S
32
Q

Isocarboxazid

MOA?

A
  • Irreversible MAO I
33
Q

Trazodone

MOA

what gives it the Serotonin activity?

Class?

A
  • phenylpiperazine
  • 5HT uptake inhibitor
  • 5HT2A antagonist
  • Sedation
  • Piperazine with phenyl CL gives serotonin activity

Medicinal Chem (15 decks)

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