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LUMC Antidepressants
Psychiatry Clerkship Antidepressant Notes
| Question | Answer |
|---|---|
| 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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