Antidepressants/Stimulants

• Mood disorders are related to alterations in levels of SER and NE
• *Low levels = depression
• *High levels = mania

• TCA: most effective for pt severely dep
• SSRIs: drug of choice for mod dep pts
• Atypical antidep
• MAOI: historically 1st to be used now limited due to side effects

• Lithium salts (carbonate and citrate)
• Antidep(fluoxetine w/olanzapine)
• Antipsychotics (risperidone, olanzapine, quetiapine)
• Anticonvulsants (valproic acid, carbamazepine, lamotrigine)

• orally active
• readily absorbed, sm int
• therapeutic effect req >2wks
• highly lipid soluble- penetrates CNS
• long 1/2 life - 5-40 hrs
• high plasma protein binding
• met by liver
• elimated by kidneys

• LOTS
• Major = CV: cardiac over + (tachycardia), slowing of A-V conductance

• Most widely used, fewer side effects
• *- of uptake achieved rapidly (w/in hrs); however mood improvement occurs after more than 2 wks b/c + neurogenesis

• orally active
• readily absorbed, sm int
• high 1st pass hepatic met
• therapeutic effect req >2wks
• Long 1/2 life (1-3 day)
• high binding plasma proteins
• Block several liver enzymes = drug interactions
• eliminated by kidney

• Early: nausea, anxiety, sleep disturbance/insomnia
• Late: anorexia, sexual dysfunction, induction of mania in pts w/bipolar

Block several liver P450 enzymes: TCA, neuroleptics (haloperidol), antiarrhythmics, some beta-adrenorec antag

• Bupropion: - DA reuptake (bipolar)
• Venlafaxine: - Ser and NE reuptake
• Nefazodone: - Ser reuptake and 5-HT2 rec
• Mirtazapine: inc NE and Ser release by blocking alpha-2 rec

• headache, nausea, tinnitus, insomnia, nervousness
• fewer than TCA, often combo w/TCA, similar TI as TCAs and SSRIs

limited due to severe and often unpredictable side effects

• oral
• transdermal patch: selegiline
• therapeutic effect req 2-4 wks
• eliminated via kidney
• blocks MAO IRREV: activity persists long after drug met and eliminated

• Lots, severe, unpredictable
• *elevated tyramine (met by MAOI) will cause release of lg amts of catecholamines ->HTN, cardia arrhythmias, stroke, headache, nausea

• Drug of choice bipolar
• onset several wks (3-4(
• will substitute for Na and produce undesirable effects
• very toxic - extremely low TI

• oral
• rapid absorption from GI
• soluble ion
• peak plasma 2-4 hrs, 1/2 life 20-24 hrs
• eliminated by kidney
• reduced kidney function w/toxicity

• CNS: tremors, mental confusion, convulsions, coma
• CV: arrythmias

• Amphetamine and its derivatives: amphetamine, dextroamphetamine, methylphenidate
• Tx: ADHD and Narcolepsy
• MOA: act by inc release of DA and NE in brain
• Numerouse side effects
• Other drugs: atomoxetine (ADHD, not +), Modafinil (narcolepsy)

• DRUG OF CHOICE FOR MAINTENANCE TX OF BIPOLAR
• alone or in combo w/antidep, neuroleptics and antiepileptics
• EXTREMELY low TI

• THIRD LINE DRUG for dep in pt resistant to other antidep
• inc presynaptic [MA] by blocking MAO
• Phenelzine, tranycypromine, selegiline, transdermal
• when combo w/SSRIs may lead to SER syndrome
• Restrictions in diet: tyramine-free food (cheese-effect)

• Heterogenous group of drugs to tx dep
• inc NE and 5HT synaptic transmission in brain
• Therapeutic efficacy similar to TCA and SSRIs
• Less toxic overall compared to TCA
• Bupropion, mirtazapine, venlafaxin, nefazodone

• FIRST LINE DRUG FOR TX DEP
• fewer side effects than TCA
• Fluoxetine, citalopram, escitalopram, sertaline

• Bloock reuptake of SER and NE
• Also block muscarinic, adrenergic, and HIS rec
• Amitriptyline, imipramine, nortriptyline, amoxapine
• Numerous side effects

• CNS: Euphoria, anxiety, vertigo, insomnia, confusion
• *Paranoia, psychoses, suicidal/homicidal impulses
• CV: Arrhythmias, HTN
• GI: Nausea, Diarrhea
• **POTENTIAL FOR ADDICTION