Antidepressants Flashcards
Fluoxetine
Selective serotonin reuptake inhibitor (SSRI)
Selective serotonin reuptake inhibitors (SSRIs)
Fluoxetine Citalopram Escitalopram Paroxetine Sertraline
Citalopram
Selective serotonin reuptake inhibitor (SSRI)
Escitalopram
Selective serotonin reuptake inhibitor (SSRI)
Paroxetine
Selective serotonin reuptake inhibitor (SSRI)
Sertraline
Selective serotonin reuptake inhibitor (SSRI)
Selective serotonin reuptake inhibitor (SSRI)
Mechanism of action
Highly selective blockade of serotonin transporter (SERT), little effect on norepinephrine transporter (NET)
Highly selective blockade of serotonin transporter (SERT), little effect on norepinephrine transporter (NET)
Selective serotonin reuptake inhibitor (SSRI)
Mechanism of action
Selective serotonin reuptake inhibitor (SSRI)
Effects
Acute increase of serotonergic synaptic activity, slower changes in several signaling pathways and neurotrophic activity
Acute increase of serotonergic synaptic activity, slower changes in several signaling pathways and neurotrophic activity
Selective serotonin reuptake inhibitor (SSRI)
Effects
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)
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
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)
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
Serotonin-norepinepherine reuptake inhibitors (SNRIs)
Duloxetine
Venlafaxine
Duloxetine
Serotonin-norepinepherine reuptake inhibitor (SNRI)
Venlafaxine
Serotonin-norepinepherine reuptake inhibitor (SNRI)
Duloxetine
Venlafaxine
Mechanism of action
Moderately selective blockade of NET and SERT
Moderately selective blockade of NET and SERT
Duloxetine
Venlafaxine
Mechanism of action
Duloxetine
Venlafaxine
Effects
Acute increase of serotonergic and adrenergic synaptic activity, otherwise like SSRIs
Acute increase of serotonergic and adrenergic synaptic activity, otherwise like SSRIs
Duloxetine
Venlafaxine
Effects
Duloxetine
Venlafaxine
Clinical applications
Major depression, chronic pain disorders, fibromyalgia, perimenopausal symptoms
Major depression, chronic pain disorders, fibromyalgia, perimenopausal symptoms
Duloxetine
Venlafaxine
Clinical applications
SNRIs
Pharmacokinetics, Toxicities, Interactions
TOXICITY: Anticholinergic, sedation, hypertension (venlafaxine) INTERACTIONS: Some CYP2D6 inhibition (duloxetine, desvenlafaxine)
TOXICITY: Anticholinergic, sedation, hypertension (venlafaxine) INTERACTIONS: Some CYP2D6 inhibition (duloxetine, desvenlafaxine)
SNRIs
Pharmacokinetics, Toxicities, Interactions
Tricyclic antidepressants (TCAs)
Imipramine
Many others
Imipramine
Tricyclic antidepressant (TCA)
Imipramine (TCA)
Mechanism of action
Mixed and variable blockade of NET and SERT
Mixed and variable blockade of NET and SERT
Imipramine (TCA)
Mechanism of action
Imipramine (TCA)
Effects
Like SNRIs plus significant blockade of autonomic nervous system and histamine receptors
Like SNRIs plus significant blockade of autonomic nervous system and histamine receptors
Imipramine (TCA)
Effects
Imipramine (TCA)
Clinical applications
Major depression not responsive to other drugs, chronic pain disorders, incontinence, obsessive-compulsive disorder (clomipramine)
Major depression not responsive to other drugs, chronic pain disorders, incontinence, obsessive-compulsive disorder (clomipramine)
Imipramine (TCA)
Clinical applications
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
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
5-HT2 antagonists
Nefazodone
Trazodone
Nefazodone
5-HT2 antagonist
Trazodone
5-HT2 antagonist
Nefazodone
Trazodone
Mechanism of action
Inhibition of 5-HT2A receptor, nefazodone also blocks SERT weakly
Inhibition of 5-HT2A receptor, nefazodone also blocks SERT weakly
Nefazodone
Trazodone
Mechanism of action
Nefazodone
Trazodone
Effects
Trazodone forms a metabolite (m-cpp) that blocks 5-HT2A,2C receptors
Trazodone forms a metabolite (m-cpp) that blocks 5-HT2A,2C receptors
Nefazodone
Trazodone
Effects
Nefazodone
Trazodone
Clinical applications
Major depression, sedation and hypnosis (trazodone)
Major depression, sedation and hypnosis (trazodone)
Nefazodone
Trazodone
Clinical applications
Nefazodone
Trazodone
Pharmacokinetics, Toxicities, Interactions
Relatively short half-lives, active metabolites, TOXICITY: Modest Alpha-and H1-receptor blockade (trazodone) INTERACTIONS: Nefazodone inhibits CYP3A4
Relatively short half-lives, active metabolites, TOXICITY: Modest Alpha-and H1-receptor blockade (trazodone) INTERACTIONS: Nefazodone inhibits CYP3A4
Nefazodone
Trazodone
Pharmacokinetics, Toxicities, Interactions
Tetracyclics, unicyclic
Bupropion
Amoxapine
Maprotiline
Mirtazapine
Bupropion
Tetracyclics, unicyclic
Amoxapine
Tetracyclics, unicyclic
Maprotiline
Tetracyclics, unicyclic
Mirtazapine
Tetracyclics, unicyclic
Mirtazapine
Bupropion
Mechanism of action
Increased norepinephrine and dopamine activity (bupropion)
NET>SERT inhibition ( amoxapine, maprotiline) increased release of norepinephrine, 5-HT (mirtazapine)
Increased norepinephrine and dopamine activity (bupropion)
NET>SERT inhibition ( amoxapine, maprotiline) increased release of norepinephrine, 5-HT (mirtazapine)
Mirtazapine
Bupropion
Mechanism of action