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Antidepressants Flashcards

0
Q

Fluoxetine

A

Selective serotonin reuptake inhibitor (SSRI)

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1
Q

Selective serotonin reuptake inhibitors (SSRIs)

A 
Fluoxetine
Citalopram
Escitalopram
Paroxetine
Sertraline
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2
Q

Citalopram

A

Selective serotonin reuptake inhibitor (SSRI)

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3
Q

Escitalopram

A

Selective serotonin reuptake inhibitor (SSRI)

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4
Q

Paroxetine

A

Selective serotonin reuptake inhibitor (SSRI)

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5
Q

Sertraline

A

Selective serotonin reuptake inhibitor (SSRI)

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6
Q

Selective serotonin reuptake inhibitor (SSRI)

Mechanism of action

A

Highly selective blockade of serotonin transporter (SERT), little effect on norepinephrine transporter (NET)

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7
Q

Highly selective blockade of serotonin transporter (SERT), little effect on norepinephrine transporter (NET)

A

Selective serotonin reuptake inhibitor (SSRI)

Mechanism of action

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8
Q

Selective serotonin reuptake inhibitor (SSRI)

Effects

A

Acute increase of serotonergic synaptic activity, slower changes in several signaling pathways and neurotrophic activity

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9
Q

Acute increase of serotonergic synaptic activity, slower changes in several signaling pathways and neurotrophic activity

A

Selective serotonin reuptake inhibitor (SSRI)

Effects

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10
Q

Selective serotonin reuptake inhibitor (SSRI)

Clinical applications

A

Major depression, anxiety disorders, panic disorder, obsessive-compulsive disorder, post-traumatic stress disorder, perimenopausal vasomotor symptoms, eating disorder (bulimia)

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11
Q

Major depression, anxiety disorders, panic disorder, obsessive-compulsive disorder, post-traumatic stress disorder, perimenopausal vasomotor symptoms, eating disorder (bulimia)

A

Selective serotonin reuptake inhibitor (SSRI)

Clinical applications

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12
Q

Selective serotonin reuptake inhibitor (SSRI)

Pharmacokinetics, Toxicities, Interactions

A

Half-lives from 15-74 h, oral activity, TOXICITY: well tolerated but cause sexual dysfunction, risk of serotonin syndrome with MAOs, INTERACTIONS: some CYP inhibition (fluoxetine 2D6, 3A4; fluvoxamine 1A2; paroxetine 2D6)

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13
Q

Half-lives from 15-74 h, oral activity, TOXICITY: well tolerated but cause sexual dysfunction, risk of serotonin syndrome with MAOs, INTERACTIONS: some CYP inhibition (fluoxetine 2D6, 3A4; fluvoxamine 1A2; paroxetine 2D6)

A

Selective serotonin reuptake inhibitor (SSRI)

Pharmacokinetics, Toxicities, Interactions

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14
Q

Serotonin-norepinepherine reuptake inhibitors (SNRIs)

A

Duloxetine

Venlafaxine

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15
Q

Duloxetine

A

Serotonin-norepinepherine reuptake inhibitor (SNRI)

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16
Q

Venlafaxine

A

Serotonin-norepinepherine reuptake inhibitor (SNRI)

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17
Q

Duloxetine
Venlafaxine

Mechanism of action

A

Moderately selective blockade of NET and SERT

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18
Q

Moderately selective blockade of NET and SERT

A

Duloxetine
Venlafaxine

Mechanism of action

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19
Q

Duloxetine
Venlafaxine

Effects

A

Acute increase of serotonergic and adrenergic synaptic activity, otherwise like SSRIs

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20
Q

Acute increase of serotonergic and adrenergic synaptic activity, otherwise like SSRIs

A

Duloxetine
Venlafaxine

Effects

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21
Q

Duloxetine
Venlafaxine

Clinical applications

A

Major depression, chronic pain disorders, fibromyalgia, perimenopausal symptoms

22
Q

Major depression, chronic pain disorders, fibromyalgia, perimenopausal symptoms

A

Duloxetine
Venlafaxine

Clinical applications

23
Q

SNRIs

Pharmacokinetics, Toxicities, Interactions

A

TOXICITY: Anticholinergic, sedation, hypertension (venlafaxine) INTERACTIONS: Some CYP2D6 inhibition (duloxetine, desvenlafaxine)

24
TOXICITY: Anticholinergic, sedation, hypertension (venlafaxine) INTERACTIONS: Some CYP2D6 inhibition (duloxetine, desvenlafaxine)
SNRIs Pharmacokinetics, Toxicities, Interactions
25
Tricyclic antidepressants (TCAs)
Imipramine | Many others
26
Imipramine
Tricyclic antidepressant (TCA)
27
Imipramine (TCA) Mechanism of action
Mixed and variable blockade of NET and SERT
28
Mixed and variable blockade of NET and SERT
Imipramine (TCA) Mechanism of action
29
Imipramine (TCA) Effects
Like SNRIs plus significant blockade of autonomic nervous system and histamine receptors
30
Like SNRIs plus significant blockade of autonomic nervous system and histamine receptors
Imipramine (TCA) Effects
31
Imipramine (TCA) Clinical applications
Major depression not responsive to other drugs, chronic pain disorders, incontinence, obsessive-compulsive disorder (clomipramine)
32
Major depression not responsive to other drugs, chronic pain disorders, incontinence, obsessive-compulsive disorder (clomipramine)
Imipramine (TCA) Clinical applications
33
Imipramine (TCA) Pharmacokinetics, Toxicities, Interactions
Long half-lives, CYP substrates, active metabolites, TOXICITY: Anticholinergic, Alpha-blocking effects, sedation, weight gain, arrhythmias, and seizures in overdose, INTERACTIONS: CYP inducers and inhibitors
34
Long half-lives, CYP substrates, active metabolites, TOXICITY: Anticholinergic, Alpha-blocking effects, sedation, weight gain, arrhythmias, and seizures in overdose, INTERACTIONS: CYP inducers and inhibitors
Imipramine (TCA) Pharmacokinetics, Toxicities, Interactions
35
5-HT2 antagonists
Nefazodone | Trazodone
36
Nefazodone
5-HT2 antagonist
37
Trazodone
5-HT2 antagonist
38
Nefazodone Trazodone Mechanism of action
Inhibition of 5-HT2A receptor, nefazodone also blocks SERT weakly
39
Inhibition of 5-HT2A receptor, nefazodone also blocks SERT weakly
Nefazodone Trazodone Mechanism of action
40
Nefazodone Trazodone Effects
Trazodone forms a metabolite (m-cpp) that blocks 5-HT2A,2C receptors
41
Trazodone forms a metabolite (m-cpp) that blocks 5-HT2A,2C receptors
Nefazodone Trazodone Effects
42
Nefazodone Trazodone Clinical applications
Major depression, sedation and hypnosis (trazodone)
43
Major depression, sedation and hypnosis (trazodone)
Nefazodone Trazodone Clinical applications
44
Nefazodone Trazodone Pharmacokinetics, Toxicities, Interactions
Relatively short half-lives, active metabolites, TOXICITY: Modest Alpha-and H1-receptor blockade (trazodone) INTERACTIONS: Nefazodone inhibits CYP3A4
45
Relatively short half-lives, active metabolites, TOXICITY: Modest Alpha-and H1-receptor blockade (trazodone) INTERACTIONS: Nefazodone inhibits CYP3A4
Nefazodone Trazodone Pharmacokinetics, Toxicities, Interactions
46
Tetracyclics, unicyclic
Bupropion Amoxapine Maprotiline Mirtazapine
47
Bupropion
Tetracyclics, unicyclic
48
Amoxapine
Tetracyclics, unicyclic
49
Maprotiline
Tetracyclics, unicyclic
50
Mirtazapine
Tetracyclics, unicyclic
51
Mirtazapine Bupropion Mechanism of action
Increased norepinephrine and dopamine activity (bupropion) | NET>SERT inhibition ( amoxapine, maprotiline) increased release of norepinephrine, 5-HT (mirtazapine)
52
Increased norepinephrine and dopamine activity (bupropion) | NET>SERT inhibition ( amoxapine, maprotiline) increased release of norepinephrine, 5-HT (mirtazapine)
Mirtazapine Bupropion Mechanism of action

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