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Flashcards in Antidepressants Deck (53):
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Selective serotonin reuptake inhibitors (SSRIs)

Fluoxetine
Citalopram
Escitalopram
Paroxetine
Sertraline

1

Fluoxetine

Selective serotonin reuptake inhibitor (SSRI)

2

Citalopram

Selective serotonin reuptake inhibitor (SSRI)

3

Escitalopram

Selective serotonin reuptake inhibitor (SSRI)

4

Paroxetine

Selective serotonin reuptake inhibitor (SSRI)

5

Sertraline

Selective serotonin reuptake inhibitor (SSRI)

6

Selective serotonin reuptake inhibitor (SSRI)

Mechanism of action

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

7

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

Selective serotonin reuptake inhibitor (SSRI)

Mechanism of action

8

Selective serotonin reuptake inhibitor (SSRI)

Effects

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

9

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

Selective serotonin reuptake inhibitor (SSRI)

Effects

10

Selective serotonin reuptake inhibitor (SSRI)

Clinical applications

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

11

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

Selective serotonin reuptake inhibitor (SSRI)

Clinical applications

12

Selective serotonin reuptake inhibitor (SSRI)

Pharmacokinetics, Toxicities, Interactions

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)

13

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)

Selective serotonin reuptake inhibitor (SSRI)

Pharmacokinetics, Toxicities, Interactions

14

Serotonin-norepinepherine reuptake inhibitors (SNRIs)

Duloxetine
Venlafaxine

15

Duloxetine

Serotonin-norepinepherine reuptake inhibitor (SNRI)

16

Venlafaxine

Serotonin-norepinepherine reuptake inhibitor (SNRI)

17

Duloxetine
Venlafaxine

Mechanism of action

Moderately selective blockade of NET and SERT

18

Moderately selective blockade of NET and SERT

Duloxetine
Venlafaxine

Mechanism of action

19

Duloxetine
Venlafaxine

Effects

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

20

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

Duloxetine
Venlafaxine

Effects

21

Duloxetine
Venlafaxine

Clinical applications

Major depression, chronic pain disorders, fibromyalgia, perimenopausal symptoms

22

Major depression, chronic pain disorders, fibromyalgia, perimenopausal symptoms

Duloxetine
Venlafaxine

Clinical applications

23

SNRIs

Pharmacokinetics, Toxicities, Interactions

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