Drug List 10: Moa [Pharmacology I]

Front 1

Mechanism of Action for Amitriptyline (a mee trip’ ti leen)

Back 1

Amitriptyline is a tricyclic antidepressant. It inhibits reuptake of serotonin and norepinephrine by blocking SERT and NET, thus facilitating their accumulation in the synaptic cleft. Many untoward effects are associated with its additional affinity for receptors of histamine, acetylcholine, and adrenaline.

Front 2

Mechanisms of Action for Clomipramine (kloe mi’ pra meen)

Back 2

Clomipramine is a tricyclic antidepressant noted for being a relatively selective inhibitor of SERT. It is noted for treatment of OCD and for causing adverse sexual side effects.

Front 3

Mechanisms of Action for Doxepin (dox’ e pin)

Back 3

Doxepin is a tricyclic antidepressant. It is noted as a potent antagonist of histamine H1 receptors, lending it to clinical use as a hypnotic and in the treatment of pruritus.

Front 4

Mechanisms of Action for Imipramine (im ip’ ra meen)

Back 4

Imipramine is a tricyclic antidepressant. It is noted for being highly anticholinergic and for being a relatively strong inhibitor of SERT and NET, having more serotonin effect initially, though its metabolite, desipramine, later balances this effect with more NET inhibition.

Front 5

Mechanism of Action for Trimipramine Maleate (trye mi’ pra meen)

Back 5

Trimipramine Maleate is a tricyclic antidepressant. It inhibits reuptake of serotonin and norepinephrine by blocking SERT and NET, thus facilitating their accumulation in the synaptic cleft. Many untoward effects are associated with its additional affinity for receptors of histamine, acetylcholine, and adrenaline.

Front 6

Mechanism of Action for Amoxapine (a mox’ a peen)

Back 6

Amoxapine is a tetracyclic antidepressant (TeCA). It is a potent NET inhibitor and a less potent inhibitor of SERT. Amoxapine is also noted for having anticholinergic and antihistaminic properties, and as a moderate inhibitor of postsynaptic D2 receptor, giving it antipsychotic properties and an association with parkinsonian syndrome.

Front 7

Mechanism of Action for Desipramine (des ip’ ra meen)

Back 7

Desipramine is a tricyclic antidepressant. It is noted for being much less anticholinergic and for being a more selective and potent inhibitor of NET.

Front 8

Mechanism of Action for Nortriptyline (nor trip’ ti leen)

Back 8

Nortriptyline is a tricyclic antidepressant noted for being a relatively selective inhibitor of NET. It is also helpful in smoking cessation (though not as consistently so as bupropion).

Front 9

Mechanism of Action for Protriptyline (proe trip’ ti leen)

Back 9

Protriptyline is a tricyclic antidepressant. It inhibits the reuptake of serotonin and norepinephrine by blocking SERT and NET, thus facilitating their accumulation in the synaptic cleft. Many untowards effects are associated with its additional affinity for receptors of histamine, acetylcholine, and adrenaline.

Front 10

Mechanism of Action for Bupropion (byoo proe’ pee on)

Back 10

Bupropion is a unicyclic antidepressant. Bupropion and its major metabolite, hydroxybupropion, are noted for modest-to-moderate inhibition of NET and DAT, and for increasing presynaptic release of NE and, to a lesser extent, DA. Bupropion is valued as an aid for smoking cessation and weight loss, and for not having sexual side effects.

Front 11

Mechanism of Action for Mirtazapine (mir taz’ a peen)

Back 11

Mirtazapine is a tetracyclic antidepressant (TeCA) that enhances the release of NE and 5-HT by antagonizing presynaptic, alpha2-autoreceptors. It also antagonizes 5-HT2 and 5-HT3 receptors and is a potent H1 antagonist, which is responsible for its sedative effect and its efficacy as a hypnotic. It is noted for not having sexual side effects.

Front 12

Mechanism of Action for Maprotiline (ma proe’ ti leen)

Back 12

Maprotiline is a tetracyclic antidepressant (TeCA). It is a potent NET inhibitor and a less potent inhibitor of SERT. It is noted for its anticholinergic and antihistaminic properties.

Front 13

Mechanism of Action for Trazodone (traz’ oh done)

Back 13

Trazodone is a potent 5-HT2A receptor antagonist associated with substantial antianxiety, antipsychotic, and antidepressant effects. It is a weak, but selective, inhibitor of SERT, and also has weak-to-moderate alpha-adrenergic blocking properties. Trazodone is also a modest antagonist of H1 receptors, leading to a highly sedating effect that is exploited for hypnotic application.

Front 14

Mechanism of Action for Nefazodone (nef ay’ zoe done)

Back 14

Nefazodone is a potent 5-HT2A receptor antagonist associated with substantial antianxiety, antipsychotic, and antidepressant effects. It is a weak inhibitor of both SERT and NET, and also has alpha-adrenergic blocking properties. Nefazodone is noted for cases of lethal hepatic failure and for not having sexual side effects.

Front 15

Mechanism of Action for Venlafaxine (ven’ la fax een)

Back 15

Venlafaxine is a selective serotonin-norepinephrine reuptake inhibitor (SNRI). It selectively binds and inhibits SERT and NET. Like most SNRIs, it has a higher affinity for SERT than NET. Venlafaxine is noted for having the lowest protein binding of all antidepressants (27%).

Front 16

Mechanism of Action for Desvenlafaxine (des ven” la fax’ een)

Back 16

Desvenlafaxine is a selective serotonin-norepinephrine reuptake inhibitor (SNRI). It is the CYP2D6 metabolite of venlafaxine, and is a more balanced inhibitor of SERT and NET than venlafaxine, which favors SERT inhibition. Desvenlafaxine is noted for having one of the lowest protein bindings of an antidepressant (30%).

Front 17

Mechanism of Action for Duloxetine (doo lox’ e teen)

Back 17

Duloxetine is a selective serotonin-norepinephrine reuptake inhibitor (SNRI). It is a relatively balanced inhibitor of SERT and NET.

Front 18

Mechanism of Action for Phenelzine (fen’ el zeen)

Back 18

The hydrazine derivative phenelzine nonselectively and irreversibly inhibits both MAO-A & MAO-B, thereby increasing catecholamine levels by blocking catecholamine degradation. Phenelzine is noted for being more sedating than selegiline or tranylcypromine.

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Mechanism of Action for Tranylcypromine (tran il sip’ roe meen)

Back 19

Tranylcypromine nonselectively and irreversibly inhibits both MAO-A & MAO-B, thereby increasing catecholamine levels by blocking catecholamine degradation.

Front 20

Mechanism of Action for Selegiline (se le’ ji leen)

Back 20

Selegiline is, at low doses, a selective, irreversible, MAO-B inhibitor, used for the treatment of Parkinson’s disease.

Front 21

Mechanism of Action for Milnacipran (mil na’ sip ran)

Back 21

Milnacipran is a selective serotonin-norepinephrine reuptake inhibitor (SNRI). It is a relatively balanced inhibitor of SERT and NET.

Front 22

Mechanism of Action for Isocarboxazid (eye soe kar box’ azid)

Back 22

The hydrazine derivative isocarboxazid nonselectively and irreversibly inhibits both MAO-A & MAO-B, thereby increasing catecholamine levels by blocking catecholamine degradation.

Front 23

Mechanism of Action for Fluoxetine (floo ox’ e teen)

Back 23

Fluoxetine is a selective serotonin reuptake inhibitor, i.e. it selectively inhibits SERT. It is noted for having the longest half-life of all SSRIs and for being a potent inhibitor of CYP2D6.

Front 24

Mechanism of Action for Paroxetine (pa rox’ e teen)

Back 24

Paroxetine is a selective serotonin reuptake inhibitor, i.e. it selectively inhibits SERT. It is noted for causing weight gain and for being a potent inhibitor of CYP2D6. Discontinuation syndrome is possible due to its short half-life.

Front 25

Mechanism of Action for Citalopram (sye tal’ oh pram)

Back 25

Citalopram is a selective serotonin reuptake inhibitor, i.e. it selectively inhibits SERT. It is noted for having only modest CYP interactions.

Front 26

Mechanism of Action for Escitalopram (es sye tal’ oh pram)

Back 26

Escitalopram is a selective serotonin reuptake inhibitor, i.e. it selectively inhibits SERT. It is the S enantiomer of citalopram and is noted for having only modest CYP interactions.

Front 27

Mechanism of Action for Sertraline (ser’ tra leen)

Back 27

Sertraline is a selective serotonin reuptake inhibitor, i.e. it selectively inhibits SERT. It is noted for having only modest CYP interactions. Discontinuation syndrome is possible due to its short half-life.

Front 28

Mechanism of Action for Fluvoxamine (floo vox’ a meen)

Back 28

Fluvoxamine is a selective serotonin reuptake inhibitor, i.e. it selectively inhibits SERT. It is noted as an inhibitor of CYP3A4.