Mood Stabilizers Flashcards
Tranylcypromine:
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
Moclobemide:
Competitive (reversible) MAO-A inhibitor
T1/2= 2 hours
-Increases 5-HT and NE in the brain WITHOUT affecting blood tyramine levels
AE’s of MAO-Inhibitors:
- CNS excitation
- Suppression of REM sleep
- Hepatotoxicity
- Serotonin syndrome
- Possible wine- cheese reaction
Imipramine:
-Tricyclic antidepressant
-Non-selective 5-HT and NE re-uptake inhibitor
T1/2= 17 hours
-may cause memory loss/ postural hypotension
Amitriptyline:
Tricyclic Antidepressant
-Non selective 5-HT and NE re-uptake inhibitor
T1/2= 38 hours
-May cause memory loss/ postural hypotension
Fluoxetine (Prozac):
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.
Fluvoxamine:
T1/2= 15 hours
Selective Serotonin Reuptake Inhibitor (SSRI)
Paroxetine:
Selective Serotonin Reuptake Inhibitor (SSRI)
T1/2= 24 hours
*lacks active metabolites
-Has less serious p450 DDIs than fluoxetine
Sertraline (Zoloft):
Selective Serotonin Reuptake Inhibitor (SSRI)
T1/2= 26 hours
Citalopram (Celexa):
Selective Serotonin Reuptake Inhibitor (SSRI)
T1/2= 35 hours
Desipramine:
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
Nortripytline:
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
Maprotiline:
Selective NE Reuptake Inhibitor
T1/2= 36 hours
-Tetracycline antidepressant
-Side effects similar to tricyclic antidepressants
Amoxapine:
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)
Nefazodone:
Atypical Antidepressant T/2= 3-4 hours *HIGH POTENCY* -Selective NE re-uptake inhibitor (5-HT2A) -Can be hepatotoxic
Bupropion:
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
Mirtazapine:
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
Lithium:
-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
Carbamazepine:
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
Valproic Acid:
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
Lamotrigine:
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
Olanzapine, Risperidone & Aripirazole
Atypical Antidepressants
- Can be used to treat acute mania/ mixed episodes
- May be required to suppress delusions/ psychotic symptoms accompanying mania
Olanzapine + Fluoxetine
- Antidepressant Monotherapy may induce mania
- Combination therapy of Olanzapine + Fluoxetine is acceptable for avoiding mania
