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LUMC Antidepressants

Psychiatry Clerkship Antidepressant Notes

QuestionAnswer
MAOIs: Generics Isocarboxazid Moclobemide Phenelzine Selegiline Tranylcypromine
TCAs: Tertiary Generics & Trades Amitriptyline (Elavil) Clomipramine (Anafranil) Doxepin (Adapin) Imipramine (Trofranil) Trimipramine (Surmontil)
SSRIs: Generics & Trades Fluoxetine (Prozac) Sertraline (Zoloft) Paroxetine (Paxil) Citalopram (Celexa) Escitalopram (Lexapro) Fluvoxamine (Luvox)
Monoamine Hypothesis/Receptor Hypothesis of Depression Depletion of monoamines in synaptic cleft & compensatory upgrading of post synaptic recepto
Raphe Nucleus: Function Serotonergic projections
Locus Ceruleus: Function Norepinephrine projections
Raphe Nucleus --> Frontal Cortex Regulates mood
Raphe Nucleus --> Basal Ganglia Regulates movement; depletion leads to OBSESSIONS & COMPULSIONS
Raphe Nucleus --> Limbic System Prevents anxiety
Raphe Nucleus --> Hypothalamus Regulates appetite
Raphe Nucleus --> Sleep centers Regulates slow wave sleep
Raphe Nucleus --> Spinal Cord Sexual side effects like delayed ejaculation
Raphe Nucleus --> Chemoreceptor trigger zone Nausea/vomiting through 5HT3 receptors
Raphe Nucleus --> Gastrointestinal Tract Diarrhea/abdominal cramps through 5HT3/4 receptors
Locus Ceruleus --> Frontal Cortex Regulates mood & cognitive functions like attention, concentration, & memory
Locus Ceruleus --> Cerebellum Causes tremors
Locus Ceruleus --> CVS Center HTN
Locus Ceruleus --> Heart (Sympathetics) Tachycardia
Locus Ceruleus --> Bladder Urinary Retention
MAOIs: MOA Inhibit monoamine oxidase enzyme which degrades Dopamine, NE, & Serotonin
MAOIs: Irreversible Will have "cheese effect" with tyramine rich food which can lead to a hypertensive crisis
MAOIs: Reversible Will NOT have tyramine effect
MAOIs: Side effects 1. Alpha 1 Blockade: orthostatic hypotension, dizziness, reflex tachycardia 2. Hisatminic: sedation & weight gain 3. MAOI diet (overdose): can lead to arrhythmias & renal failure
MAOIs: Considerations Start SSRI only after 2-4 weeks of d/c MAOIs
TCAs: MOA Block reuptake of NE, 5HT, DA & increase their levels. *Also interact with muscarinic, histamine, & alpha adrenergic receptors
TCAs: Indications Second line for depression & anxiety, pain syndromes, neuropathic pain, insomnia, and sometimes in ADHD
TCAs: Side Effects Alpha adrenergic: orthostatic hypotension, dizziness, reflex tachycardia Anticholinergic: blurred vision, constipation, urinary retention, glaucoma Cardiac Toxicity, Seizures, Tremor, Ataxia Sedation
SSRIs: MOA Selectivel block neuronal reuptake of 5HT (Serotonin). Doing this increases levels of 5-HT which later leads to down-regulation of post synaptic receptors. Onset of action is delayed by 4-6 weeks because 2nd messenger systems must be activated
SSRIs: Side Effects - GI nausea, diarrhea, anorexia, vomiting - Sedation, insomnia, vivid dreams - Weight gaine - Agitation, anxiety (in pt w/ anxiety) - Sexual side effects in 20-30%
SNRIs: MOA Have dual action and block reuptake of both NE & 5HT. Examples: Venlafaxine (Effexor), Desvenlafaxine (Pristiq), Duloxetine (Cymbalta)
Fluoxetine aka Prozac - Longest t1/2 due to active metabolites - Activating: better for ATYPICAL depression with hypersomnia/psychomotor retardation - Well studied in pregnant women
Sertraline aka Zoloft - Sedating; a good first choice - Best documented CV safety - Has additional DOPAMINE reuptake activity
Paroxetine aka Paxil - Sedating, has mild anticholinergic effects & SEs - More weight gain - Good for ANXIOUS-depression - Short t1/2 so worst withdrawal sx
Citalopram aka Celexa - Sedating due to antihistaminic action - Has less drug interactions & well tolerated - Good for use in ELDERLY due to low intxns
Escitalopram aka Lexapro - Fewer side effects/interactions than Citalopram & twice as potent
Fluvoxamine aka Luvox - Leased used d/t many drug intxns - Has shortest half life, is sedating - Good or anxious depression & treatment resistant OCD
Venlafaxine - Graded effects; Low doses --> Serotonin (75-225mg) Middle doses --> NE (225-375mg) High doses --> Dopamine (>375mg) - Good for neuropathic pain - Must monitor blood pressure due to HTN
Duloxetine aka Cymbalta -
Buproprion aka Wellbutrin, Zyban - NDRI (NE & Dopamine reuptake inhibitor) - Good for depression with fatigue, ADHD, & smoking cessation. - No effect on anxiety, no sexual dysfunction - Causes weight loss - Avoid in pts w/ ED, hx of seizures
Mirtazapine aka Remeron - Noradrenergic & Specific serotonergic antidepressant (NaSSAs) - Good for anxiety sxs & depression, is sedating, has anti-emetic effect - Use in EDs as appetite stimulant - Insomnia/activation at higher doses
Trazadone Inhibits presynaptic Serotonin reuptake, blocks postsynaptic 5HT2 receptor, & has antihistaminic properties - Sedating at low doses (50mg-100mg) - Risk of Priapism
Serotonin Syndrome - Excess serotonergic activity at CNS * periphery - Drug combos: SSRI + tramadol or linezolide - Sx: Hyperthermia, autonomic instability, rigidity, myoclonus - Tx: stop usage of precipitating drugs and give serotonin antagonists: CRYPTOHEPTADINE
Serotonin Discontinuiation Syndrome Can occur following interruption/dose reduction/discontinuation of SSRI/SNRI (esp. those w/ short t1/2) - N/V, dizziness, insomnia, irritability, shock-like sensations, parasthesias - Prevent by slow taper, subs. Prozac in final stages of SSRI discont.
Created by: dsilver2
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