Anti-Depressant/Mood Stablize

Question 1

Amitriptyline [Elavil]

Answer 1

TCA Anti-Depressant
MoA: dec presynaptic reuptake 5HT, NE -> inc transmit and change receptor profile
Use: Major Depression; !LOW TI! -> arrhyth, cardiac failure, CHF
Acute: drowsy w/ dec cognition
Chronic (2-8wks): inc cognition w/o euphoria
PK: Lipid Sol -> to fat/brain; High ProBind -> inc Vd, T1/2, dec excret; demethylation, 2D6
ADE: Block mACh, 5HT, His -> ortho-hypo/syncopy, anti-mACh effects (contra Glaucoma), sedation, weight gain, sexual disturbance
DDI: EtOH, sedatives, block Clonidine

Question 2

Imipramine [Togranil]

Answer 2

TCA Anti-Depressant
MoA: dec presynaptic reuptake 5HT, NE -> inc transmit and change receptor profile
Use: Major Depression; !LOW TI! -> arrhyth, cardiac failure, CHF
Acute: drowsy w/ dec cognition
Chronic (2-8wks): inc cognition w/o euphoria
PK: Lipid Sol -> to fat/brain; High ProBind -> inc Vd, T1/2, dec excret; demethylation, 2D6
ADE: Block mACh, 5HT, His -> ortho-hypo/syncopy, anti-mACh effects (contra Glaucoma), sedation, weight gain, sexual disturbance
DDI: EtOH, sedatives, block Clonidine

Question 3

Nortriptyline [Pamelor]

Answer 3

TCA Anti-Depressant
MoA: dec presynaptic reuptake 5HT, NE -> inc transmit and change receptor profile
Use: Major Depression; !LOW TI! -> arrhyth, cardiac failure, CHF
Acute: drowsy w/ dec cognition
Chronic (2-8wks): inc cognition w/o euphoria
PK: Lipid Sol -> to fat/brain; High ProBind -> inc Vd, T1/2, dec excret; demethylation, 2D6
ADE: Block mACh, 5HT, His -> ortho-hypo/syncopy, anti-mACh effects (contra Glaucoma), sedation, weight gain, sexual disturbance
DDI: EtOH, sedatives, block Clonidine

Question 4

Desipramine [Norpramin]

Answer 4

TCA Anti-Depressant
MoA: dec presynaptic reuptake 5HT, NE -> inc transmit and change receptor profile
Use: Major Depression; !LOW TI! -> arrhyth, cardiac failure, CHF
Acute: drowsy w/ dec cognition
Chronic (2-8wks): inc cognition w/o euphoria
PK: Lipid Sol -> to fat/brain; High ProBind -> inc Vd, T1/2, dec excret; demethylation, 2D6
ADE: Block mACh, 5HT, His -> ortho-hypo/syncopy, anti-mACh effects (contra Glaucoma), sedation, weight gain, sexual disturbance
DDI: EtOH, sedatives, block Clonidine

Question 5

Buproprion [Wellbutrin]

Answer 5

Atypical Anti-Depressant + Smoking Cessation
MoA: WEAK block D, 5HT, ME; metabolite SNRI
Admin: divided dose or slow release
ADE: Inc Monoamine -> agitation, anxiety, restlessness, Seizure

Question 6

Venlafaxine [Effexor]

Answer 6

Atypical Anti-Depressant; SNRI w/o anti-His/mACh/adrenergic effects (less than TCAs)
PK: short T1/2, must taper (avoid reflexive depression)
ADE: small sustained HTN, sweat dizzy, N, anxiety, Serotonin Syndrome

Question 7

Duloxetine [Cymbalta]

Answer 7

Atypical Anti-Depressant; Most Potent SNRI

PK: 2D6/1A2, 50%bioaval, high ProBind

Question 8

Mirtazapine [Remeron]

Answer 8

Atypical Anti-Depressant
MoA: Inc 5HT/NE release by block presynapse alpha2-AD heteroreceptor; Block 5HT-2 Receptors
ADE: potent anti-His -> sedation, weight gain

Question 9

Trazodone [Desyrel, Oleptro ER]

Answer 9

Atypical Anti-Depressant
MoA: moderate SSRI, 5HT-2a antagonist + 5HT-1 partial agonist (SARI)
Use: depression w/ anxiety + sleep disturbance
PK: short T1/2, Inh 3A4
Serotonin Syndrome

Question 10

Citalopram [Celexa]

Answer 10

SSRI Anti-Depressant (1st Line!) + anti-anxiety, panic, OCD, ADHD, eating disorders
MoA: Inh SERT -> potentiate/prolong 5HT action. Min effect @ mACh/His
Acute: CNS stimulation, anxiety, agitation
Chronic (2-6 wks): improve but stimulation remains
PK: high bioaval, high ProBind, long T1/2 (days), meta 2D6/2C19/3A4, inh 2D6/2C19
ADE (high TI): sex dysfunc, N/V -> least in general
Possible birth defects
OD (<24hrs): Serotonin Syndrome (esp.w/ MAOI)

Question 11

Escitalopram [Lexapro]

Answer 11

SSRI Anti-Depressant (1st Line!) + anti-anxiety, panic, OCD, ADHD, eating disorders
MoA: Inh SERT -> potentiate/prolong 5HT action. Min effect @ mACh/His
Acute: CNS stimulation, anxiety, agitation
Chronic (2-6 wks): improve but stimulation remains
PK: high bioaval, high ProBind, long T1/2 (days), meta 2D6/2C19/3A4, inh 2D6/2C19
ADE (high TI): sex dysfunc, N/V -> least in general
Possible birth defects
OD (<24hrs): Serotonin Syndrome (esp.w/ MAOI)

Question 12

Fluoxetine [Prozac]

Answer 12

SSRI Anti-Depressant (1st Line!) + anti-anxiety, panic, OCD, ADHD, eating disorders
MoA: Inh SERT -> potentiate/prolong 5HT action. Min effect @ mACh/His
Acute: CNS stimulation, anxiety, agitation
Chronic (2-6 wks): improve but stimulation remains
PK: high bioaval, high ProBind, meta 2D6/2C19/3A4, inh 2D6/2C19
super long T1/2 (7-9 d): norfluoxetine active metabolite -> weekly admin
ADE (high TI): sex dysfunc, N/V -> least in general
Possible birth defects
OD (<24hrs): Serotonin Syndrome (esp.w/ MAOI)

Question 13

Paroxetine [Paxil]

Answer 13

SSRI Anti-Depressant (1st Line!) + anti-anxiety, panic, OCD, ADHD, eating disorders
MoA: Inh SERT -> potentiate/prolong 5HT action. Min effect @ mACh/His
Acute: CNS stimulation, anxiety, agitation
Chronic (2-6 wks): improve but stimulation remains
PK: high bioaval, high ProBind, long T1/2 (days), meta 2D6/2C19/3A4, inh 2D6/2C19
ADE (high TI): sex dysfunc, N/V -> least in general
Birth Defects!!!
OD (<24hrs): Serotonin Syndrome (esp.w/ MAOI)

Question 14

Sertraline [Zoloft]

Answer 14

SSRI Anti-Depressant (1st Line!) + anti-anxiety, panic, OCD, ADHD, eating disorders
MoA: Inh SERT -> potentiate/prolong 5HT action. Min effect @ mACh/His
Acute: CNS stimulation, anxiety, agitation
Chronic (2-6 wks): improve but stimulation remains
PK: high bioaval, high ProBind, long T1/2 (days), meta 2D6/2C19/3A4, inh 2D6/2C19
ADE (high TI): sex dysfunc, N/V -> least in general
Possible birth defects
OD (<24hrs): Serotonin Syndrome (esp.w/ MAOI)

Question 15

Fluvoxamine [Luvox]

Answer 15

SSRI Anti-Depressant (1st Line!) + anti-anxiety, panic, OCD, ADHD, eating disorders
MoA: Inh SERT -> potentiate/prolong 5HT action. Min effect @ mACh/His
Acute: CNS stimulation, anxiety, agitation
Chronic (2-6 wks): improve but stimulation remains
PK: high bioaval, high ProBind, long T1/2 (days), meta 2D6/2C19/3A4, inh 2D6/2C19
ADE (high TI): sex dysfunc, N/V -> least in general
Possible birth defects
OD (<24hrs): Serotonin Syndrome (esp.w/ MAOI)

Question 16

Phenelzine [Nardil]

Answer 16

MAOI Anti-Depressant (last resort)
Use: ONLY if other meds fail and ECT not option
MoA: block monoamine metabolism via Irreversible Inh of MAO-A (NE/5HT/tyramine) and MAO-B (D)
Acute: CNS stim, agitation, euphoria
Chronic (2-6 wks): improve, stim remains
PK: daily dose, acetyl to inactive, inc duration due to irreversible
DDI: cheese! (tyramine), sympathomimetics (HTN), meperidine/dextromethorpham (hyperreflex, delirium, convulsion, death), SSRI (serotonin syndrome), etc…
ADE (due inc monoamine): sleep disturbance (inc arousal), OrthoHypo, weight gain, sex dysfunc, Serotonin Syndrome

Question 17

Lithium [Lithobid]

Answer 17

Mood Stabilizer (1st Line)
Use: maintenance (not acute) of manic condition, 60% effective
MoA: ??? Inh IPO3 signaling, AC signaling
PK: rapid/complete absorb -> rapid distribute w/ conc in bone, renal clear, T1/2 20hr, NO metabolism
ADE: VERY Narrow TI!! -> hit all high flow organs
tremor, ataxia, sedation, edema, hypothyroid, nephro DI, Cat D, cardio sick sinus (brady/tachy mix), acne, folliculitis, exacerbate psoriasis, Serotonin Syndrome
DDI: diuretics and NSAIDs

Question 18

Valproate/Divalproex [Depacon]

Answer 18

Mood Stabilizer/Anti-Convulsant
Use: maintenance (not acute) of manic condition alone or w/ Li or other antipsychotics
MoA (4): Inh Volt-Gate Na Channel by stable inactive state, Block Ca Channel (T-type), Stim GABA synth, Inh GABA breakdown, Inc K conductance
PK: Inh 2C9/UGT -> affect itself and many drugs
DDI: displace phenytoin plasma binding
ADE: N, ab pain, heartburn, sedation, hept tox, Serotonin Syndrome

Question 19

Carbamazepine [Tegretol]

Answer 19

Mood Stabilizer
Use: maintenance (not acute) of manic condition alone or w/ Li or other antipsychotics
MoA: Inh Volt-Gate Na Channel (prolong inactive)
PK: good absorb, ProBound/poor solub, Induce 2C/3A and UGT -> dec own conc and others
Toxic:diplopia, ataxia, GI upset, drowsiness, rash, APLASTIC Anemia

Question 20

Lamotrigine [Lamictal]

Answer 20

Mood Stabilizer
Use: maintenance (not acute) of manic condition alone or w/ Li or other antipsychotics
MoA: Inh Volt-Gate Na Channel (prolong inactive)

Question 21

Selegiline

Answer 21

MAOI Anti-Depressant (last resort)
Use: ONLY if other meds fail and ECT not option
MoA: block monoamine metabolism via Irreversible Inh of MAO-A (NE/5HT/tyramine) and MAO-B (D)
Acute: CNS stim, agitation, euphoria
Chronic (2-6 wks): improve, stim remains
PK: daily dose, acetyl to inactive, inc duration due to irreversible
DDI: cheese! (tyramine), sympathomimetics (HTN), meperidine/dextromethorpham (hyperreflex, delirium, convulsion, death), SSRI (serotonin syndrome), etc…
ADE (due inc monoamine): sleep disturbance (inc arousal), OrthoHypo, weight gain, sex dysfunc

Question 22

St. John’s Wort

Answer 22

Treat Depression?

Induces CYPs, Serotonin Syndrome