Antidepressants / Bipolar drugs

Question 1

MOA/Neurochemical Effects: Block reuptake of NE and/or 5HT
Desipramine = NE-selective
Imipramine = NE and 5HT

Higher concentration of NT at their receptors

Answer 1

Tricyclic Antidepressants
Desipramine (Norpramin)
Imipramine (Tofranil)

Question 2

Clinical Effects: Elevation in mood (2-3 wks delayed)

Causes antimuscarinic effects, sleepiness, lightheadedness in those who don’t have depression

Answer 2

Tricyclic Antidepressants
Desipramine (Norpramin)
Imipramine (Tofranil)

Question 3

AE/Toxicity: Weight gain, drowsiness, dry mouth, blurred vision, constipation, drowsiness, lightheadedness, orthostatic hypotension, arrhythmias, cardiac arrest, seizures

Answer 3

Tricyclic Antidepressants
Desipramine (Norpramin)
Imipramine (Tofranil)

Question 4

TI is low&raquo_space; lethality in overdose

Metabolized by CYP2D6 (E is inhibited by fluoxetine)

Answer 4

Tricyclic Antidepressants
Desipramine (Norpramin)
Imipramine (Tofranil)

Question 5

MOA/Neurochemical Effects: Irreversibly blocks MAO-A (NE and 5HT) and MAO-B (DA)

Increased NT in vesicles/released/action at R

Answer 5

Monoamine Oxidase Inhibitors

Phenelzine (Nardil)

Question 6

AE/Toxicity: Serotonin Syndrome (overactivation of 5HT2A  hyperthermia), potentiates sympathomimetic amines (tyramine hypertensive crisis)

Answer 6

Monoamine Oxidase Inhibitors

Phenelzine (Nardil)

Question 7

Low TI

Do not start until 14 days following discontinuation of SSRIs

Answer 7

Monoamine Oxidase Inhibitors

Phenelzine (Nardil)

Question 8

MOA/Neurochemical Effects: Blocks reuptake of 5HT from synapse (5HT2A R)  can trigger actions postsynaptically or bind to autoreceptors & inhibit more 5HT release

Answer 8

Selective Serotonin Reuptake Inhibitors
Fluoxetine (Prozac),
Sertraline (Zoloft), Escitalopram (Lexapro)

Question 9

AE/Toxicity: Nausea, diarrhea, weight loss, sexual dysfunction, anxiety, nervousness, insomnia (NOT sedating like TCAs)
Black box warning  suicide

Answer 9

Selective Serotonin Reuptake Inhibitors
Fluoxetine (Prozac),
Sertraline (Zoloft), Escitalopram (Lexapro)

Question 10

Should NOT be used alone in bipolar  can flip switch to manic

Answer 10

Selective Serotonin Reuptake Inhibitors
Fluoxetine (Prozac),
Sertraline (Zoloft), Escitalopram (Lexapro)

Question 11

MOA/Neurochemical Effects: SNRI – blocks 5HT + NE reuptake

Efficacy improves with increasing dose (increase dose: only 5HTalso NEalso DA)

Answer 11

Venlafaxine (Effexor)

Question 12

Clinical Effects: Effect on mood driven by same mechanism as TCAs but does NOT affect NE/HA/ACh R (less AE)

Answer 12

Venlafaxine (Effexor)

Question 13

AE/Toxicity: Contraindicated in patients on MAOIs

Answer 13

Venlafaxine (Effexor)

Question 14

Atypical (dual/mixed action)

May be mediated by 3 different monoamines (depends on dose)

Answer 14

Venlafaxine (Effexor)

Question 15

Blocks presynaptic α2 receptor on NE neurons (autoR) and 5HT neurons (heteroR)  increases NE and 5HT levels

Answer 15

Mirtazapine (Remeron)

Question 16

MOA/Neurochemical Effects: Injectable anesthetic, NMDA antagonist (glutamate)

Answer 16

Ketamine

Question 17

Clinical Effects: Single dose improves depression sx in 2 hrs, effects last for 1 wk

Answer 17

Ketamine

Question 18

AE/Toxicity: Nightmares and hallucinations

Answer 18

Ketamine

Question 19

AZD6765 = NMDA channel blocker with low rates of psycho AE

Answer 19

Ketamine

Question 20

Tricyclic Antidepressants

Answer 20

Desipramine (Norpramin)

Imipramine (Tofranil)

Question 21

Monoamine Oxidase Inhibitors

Answer 21

Phenelzine (Nardil)

Question 22

Selective Serotonin Reuptake Inhibitors

Answer 22

Fluoxetine (Prozac),

Sertraline (Zoloft), Escitalopram (Lexapro)

Question 23

MOA/Neurochemical Effects: Effects postsynaptic neuron – alters gene expression implicated in long-term neuroplastic events  long-term mood stabilization

Answer 23

Lithium Carbonate

Lithobid, Eskalith

Question 24

Clinical Effects: Effective in 60-80% of those with bipolar, therapeutic effect seen in 5-21 days

Prevents mood swings –increases euthymia range

Answer 24

Lithium Carbonate

Lithobid, Eskalith

Question 25

AE/Toxicity: Therapeutic: fatigue, weakness, slurred speech, ataxia, tremor, excessive thirst/urination Toxic: LOC, coma, muscular rigidity, hyperreflexia, tremor, muscle fasciculations (TI LOW)

Answer 25

Lithium Carbonate | Lithobid, Eskalith

Question 26

Tolerance to AE after 4 wks (except for tremor and urination/thirst) Renal clearance reduced 25% by diuretics

Answer 26

Lithium Carbonate | Lithobid, Eskalith

Question 27

MOA/Neurochemical Effects: Anticonvulsant

Answer 27

Valproic Acid | Depakene

Question 28

Clinical Effects: Efficacy similar to Li+, superior to Li+ for rapid-cycling bipolar

Answer 28

Valproic Acid | Depakene

Question 29

Appropriate 1st line therapy for some (can combine with Li+)

Answer 29

Valproic Acid | Depakene

Question 30

Anticonvulsant

Answer 30

Carbamazepine | Tegretol

Question 31

Prophylaxis of bipolar disorder

Answer 31

Carbamazepine | Tegretol

Question 32

Fluoxetine (Prozac), | Sertraline (Zoloft), Escitalopram (Lexapro)

Answer 32

Selective Serotonin Reuptake Inhibitors

Question 33

Phenelzine (Nardil)

Answer 33

Monoamine Oxidase Inhibitors

Question 34

Desipramine (Norpramin) | Imipramine (Tofranil)

Answer 34

Tricyclic Antidepressants