Mood Stabilizers

Question 1

Tranylcypromine:

Answer 1

Irreversible MAO-A,B inhibitor
T1/2= 2 hours (1 dose lasts about 7 days)
-Increases 5-HT, DA and NE in the brain
-Increases dietary tyramine form the gut to the bloodstream

Question 2

Moclobemide:

Answer 2

Competitive (reversible) MAO-A inhibitor
T1/2= 2 hours
-Increases 5-HT and NE in the brain WITHOUT affecting blood tyramine levels

Question 3

AE’s of MAO-Inhibitors:

Answer 3

• CNS excitation
• Suppression of REM sleep
• Hepatotoxicity
• Serotonin syndrome
• Possible wine- cheese reaction

Question 4

Imipramine:

Answer 4

-Tricyclic antidepressant
-Non-selective 5-HT and NE re-uptake inhibitor
T1/2= 17 hours
-may cause memory loss/ postural hypotension

Question 5

Amitriptyline:

Answer 5

Tricyclic Antidepressant
-Non selective 5-HT and NE re-uptake inhibitor
T1/2= 38 hours
-May cause memory loss/ postural hypotension

Question 6

Fluoxetine (Prozac):

Answer 6

Selective Serotonin Reuptake Inhibitor (SSRI)
-T1/2= 3 days
Active metabolite norfluoxetine has a longer biological half life= 7 days
-Inhibits cytochrome P450 enzyme (CYP2D6) causing potentially fatal DDI with narcotics, alcohol, ect.

Question 7

Fluvoxamine:

Answer 7

T1/2= 15 hours

Selective Serotonin Reuptake Inhibitor (SSRI)

Question 8

Paroxetine:

Answer 8

Selective Serotonin Reuptake Inhibitor (SSRI)
T1/2= 24 hours
*lacks active metabolites
-Has less serious p450 DDIs than fluoxetine

Question 9

Sertraline (Zoloft):

Answer 9

Selective Serotonin Reuptake Inhibitor (SSRI)

T1/2= 26 hours

Question 10

Citalopram (Celexa):

Answer 10

Selective Serotonin Reuptake Inhibitor (SSRI)

T1/2= 35 hours

Question 11

Desipramine:

Answer 11

Selective NE Reuptake Inhibitor
T1/2= 38 hours
-Is the active metabolite of Imipramine (17 hours)
-Has less affinity for muscarinic and alpha1 receptors than imipramine

Question 12

Nortripytline:

Answer 12

T1/2= 55 hours
Selective NE Reuptake Inhibitor
-Is the active metabolite of Amitriptyline (T=38 hours)
-Less affinity for the muscarinic and alpha1 receptors than Amitriptyline

Question 13

Maprotiline:

Answer 13

Selective NE Reuptake Inhibitor
T1/2= 36 hours
-Tetracycline antidepressant
-Side effects similar to tricyclic antidepressants

Question 14

Amoxapine:

Answer 14

Atypical Antidepressant
T1/2= 8 hours
Moderate- strong reuptake inhibitor (blocks 5-HT2A)
-Antagonist of select 5-HT, NE and DA receptors (antagonist/ inverse agonist)

Question 15

Nefazodone:

Answer 15

Atypical Antidepressant
T/2= 3-4 hours 
*HIGH POTENCY* 
-Selective NE re-uptake inhibitor (5-HT2A) 
-Can be hepatotoxic

Question 16

Bupropion:

Answer 16

Atypical Antidepressant
T1/2= 4-8 hours
Nicotinic ACh- R antagonist 
-Weak DA re-uptake inhibitor (NE swell) 
-->Effective alone, but often administered with a drug regimen to increase NE/ 5-HT for deficits

Question 17

Mirtazapine:

Answer 17

Atypical Antidepressant
T1/2= 30 hours
Blocks pre-synaptic alpha2 receptors that inhibit the release of 5-HT and NE
-Increases 5-HT and NE
(Inverse agonist/ antagonist @ 5-HT, DA and adrenergic receptors)
AE’s: Increased appetite/ weight gain

Question 18

Lithium:

Answer 18

-Treatment of Bipolar Disorder
T1/2= 8-30 hours
-Aborts manic episodes/ mildly helps depression
-Antagonizes 5-HT1A and 5-HT1B receptors, preventing feedback inhibition
-Enhances glutamate re-uptake
-Not effective in the long term due to side effects:
-Nausea, drowsiness, weight gain, fine hand tremor and polyuria
-Low therapeutic index (0.6-1.2 mg) TOXIC @ 1.4mg
-Dangerous to combine with other drugs

Question 19

Carbamazepine:

Answer 19

T1/2=15-30 hours
-Potentiates GABAergic receptor currents
-Decreases Na+ channels
-Some antidepressant/ anti-manic properties with fewer adverse effects than Lithium
AE’s: Dizziness, Ataxia & double vision

Question 20

Valproic Acid:

Answer 20

T1/2= 13-21 hours
-Decreases voltage gated Na+ channels
-Potentiates GABAergic receptor currents
-Also a histone deacetylase inhibitor (which can lead to epigenetic effects- changes in gene expression)
AE’s: Nausea, vomiting, diarrhea, headache, tremor, double vision, drowsiness and dizziness

Question 21

Lamotrigine:

Answer 21

T1/2= 13 hours

• Decreases voltage gated Na+ channels
• Blocks L, N and P type Ca2+ channels
• Weak 5-HT3 receptor inhibitor
• Inhibits glutamate release (helps stabilize mood)
• Effective in treating the depression of bipolar

-Other Na+ channel blocker’s do not work for Bipolar Disorder
AE’s: Dizziness, Ataxia and double vision

Question 22

Olanzapine, Risperidone & Aripirazole

Answer 22

Atypical Antidepressants

• Can be used to treat acute mania/ mixed episodes
• May be required to suppress delusions/ psychotic symptoms accompanying mania

Question 23

Olanzapine + Fluoxetine

Answer 23

• Antidepressant Monotherapy may induce mania

- Combination therapy of Olanzapine + Fluoxetine is acceptable for avoiding mania