Tweet
Antidepressants
• Tricyclics
– prevent reuptake of serotonin or norepinephrine/epinephrine. Block acetylcholine and histamine receptors.
• Elavil (amitryptiline), (Asendin) amoxapine, Norpramin (desipramine), Tofranil (imipramine)
• MAO Inhibitors
– block monoamine oxidase (MAO) from breaking down monoamines (serotonin, dopamine, and norepinephrine/epinephrine)
• Nardil (phenelzine), Parnate (tranylcypromine)
• SSRIs (selective serotonin reuptake inhibitors)
– Block reuptake of serotonin by presynaptic neuron
• Prozac (fluoxetine), Zoloft (setraline), Paxil (paroxetine), Celexa (citalopram)
– Increased serotonin release = sexual side effects (reduced drive and function)
• SNRI (serotonin-norepinephrine reuptake inhibitor)
– Blocks reuptake of serotonin and norepinephrine by presynaptic neuron
– Also have sexual side effects
• Cymbalta (duloxetine), Effexor (venlafaxine)
• Triple Reuptake Inhibitors (TRIs)
• New, experimental class of antidepressants. Block reuptake of dopamine, serotonin and norepinephrine
• Theoretically should have reduced sexual side effects, due to:
• Relatively lower blockade of serotonin transporters
• Enhanced availability of dopamine
• Functional TRI: take bupropion (Wellbutrin; inhibits DA and NE reuptake) plus fluoxetine (Prozac; inhibits serotonin reuptake)
• DOV 216,303: Experimental TRI in Phase II trial. Related compound (DOV 21,947) starts Phase II in January 2007.
• Atypical antidepressants
– Generally act on dopamine or norepinephrine systems, but not always serotonin
– Bupropion (Wellbutrin), maprotiline (Ludiomil), mirtazapine (Remeron)
– Wellbutrin is a reuptake inhibitor of dopamine and norepinephrine
Bipolar Disorder
• Mood Stabilizers
– Lithium: a salt that stabilizes mood by decreasing mania
• Less effective for depression (often given with an antidepressant)
• Cessation of lithium results in increased bouts of mania and increases suicide risk
• Complex mechanism of action
• Increases serotonin release
• Alters second messenger activity
• Alters neurotrophic factors
– Anticonvulsants
• Have mood-stabilizing effects
• Depakote (valproate), Tegretol (carbamazepine), Topamax (topiramate)
• Increase GABA release
– Sedatives (anxiety or insomnia)
• Benzodiazepines, e.g., Klonopin (clonazepam)
• Sleep Aids: Lunesta, Ambien
• Both the benzodiazepines, Lunesta and Ambien facilitate increased GABA neurotransmission
– Antidepressants
• Antipsychotic Drugs
• Offer mood stabilizing effects as well.
• Clozaril (clozapine), Zeprexa (olanzapine), Seroquel (quetiapine), Geodon (ziprasidone)
• Tricyclics
– prevent reuptake of serotonin or norepinephrine/epinephrine. Block acetylcholine and histamine receptors.
• Elavil (amitryptiline), (Asendin) amoxapine, Norpramin (desipramine), Tofranil (imipramine)
• MAO Inhibitors
– block monoamine oxidase (MAO) from breaking down monoamines (serotonin, dopamine, and norepinephrine/epinephrine)
• Nardil (phenelzine), Parnate (tranylcypromine)
• SSRIs (selective serotonin reuptake inhibitors)
– Block reuptake of serotonin by presynaptic neuron
• Prozac (fluoxetine), Zoloft (setraline), Paxil (paroxetine), Celexa (citalopram)
– Increased serotonin release = sexual side effects (reduced drive and function)
• SNRI (serotonin-norepinephrine reuptake inhibitor)
– Blocks reuptake of serotonin and norepinephrine by presynaptic neuron
– Also have sexual side effects
• Cymbalta (duloxetine), Effexor (venlafaxine)
• Triple Reuptake Inhibitors (TRIs)
• New, experimental class of antidepressants. Block reuptake of dopamine, serotonin and norepinephrine
• Theoretically should have reduced sexual side effects, due to:
• Relatively lower blockade of serotonin transporters
• Enhanced availability of dopamine
• Functional TRI: take bupropion (Wellbutrin; inhibits DA and NE reuptake) plus fluoxetine (Prozac; inhibits serotonin reuptake)
• DOV 216,303: Experimental TRI in Phase II trial. Related compound (DOV 21,947) starts Phase II in January 2007.
• Atypical antidepressants
– Generally act on dopamine or norepinephrine systems, but not always serotonin
– Bupropion (Wellbutrin), maprotiline (Ludiomil), mirtazapine (Remeron)
– Wellbutrin is a reuptake inhibitor of dopamine and norepinephrine
Bipolar Disorder
• Mood Stabilizers
– Lithium: a salt that stabilizes mood by decreasing mania
• Less effective for depression (often given with an antidepressant)
• Cessation of lithium results in increased bouts of mania and increases suicide risk
• Complex mechanism of action
• Increases serotonin release
• Alters second messenger activity
• Alters neurotrophic factors
– Anticonvulsants
• Have mood-stabilizing effects
• Depakote (valproate), Tegretol (carbamazepine), Topamax (topiramate)
• Increase GABA release
– Sedatives (anxiety or insomnia)
• Benzodiazepines, e.g., Klonopin (clonazepam)
• Sleep Aids: Lunesta, Ambien
• Both the benzodiazepines, Lunesta and Ambien facilitate increased GABA neurotransmission
– Antidepressants
• Antipsychotic Drugs
• Offer mood stabilizing effects as well.
• Clozaril (clozapine), Zeprexa (olanzapine), Seroquel (quetiapine), Geodon (ziprasidone)