442-MT2-Antidepressants

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Author:
jgiantess
ID:
142166
Filename:
442-MT2-Antidepressants
Updated:
2012-03-17 22:30:58
Tags:
pharmacology
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Description:
pharmacology
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  1. monoamine oxidase inhibitors
    • irreversible: phenelzine, tranylcypromine
    • reversible: moclobemide
    • - well absorbed from GI, peak levels in 2-3 hrs, metab’d in liver (acetyl), excreted in urine
    • - *precaution: hepatic or renal impairment, pregnancy and lactation
    • - NOT 1st line: resistant depression.
    • - SE: INODES
    • - overdose: sx 12 hours after ingestion: tachy, circulatory collapse, sz, coma
    • - tx of overdose: eliminate toxin via gastric lavage, urine acidification, hemodialysis
    • - DI: TCA, sympathomimetics, SSRI/SNRI, meperidin, tyramine.
  2. TCAs for depression
    • tricyclics: 2o: desi, nortrip (pref NE block). 3o: imip, amitrip, clomip, doxepin, trimip (pref 5-HT block)
    • tetracyclic: maprotiline
    • increasing NE selectivity: ami < imi < nor < maprotiline
    • - well absorbed from GI, highly PB and lipid solub, peak levels in 2-3 hrs, metab’d in liver (acetyl), excreted in urine
    • - *precaution: hepatic or renal impairment, pregnancy and lactation
    • - depression, childhood enuresis (imipramine), OCD (clomipramine), adjunctive analgesics, trigeminal neuralgia
    • - SE: antichol, antihist, antiadrenergic, sexual dysfxn, reduced sz threshold
    • - overdose: lethal. tx: activated charcoa, urine alkalinization to speed elim, life support.
    • - DI: MAOIs, barb/cbmz/rifampin induce enzymes, cimetidine/atipsychs inhibit enzymes, clonidine (dec'd anti-htn effects)
  3. SSRIs
    • citalopram, fluoxetine, fluvoxamine, paroxetine, escitalopram, sertraline
    • increasing 5-HT selectivity: clomipramine < fluoxetine < sertraline
    • - selectively inhibit human serotonin transporter (hSERT) and cause increased 5-HTP concentrations at nerve endings.
    • - little/no effect NE/DA
    • - little/no CVS effects
    • - 1st Choice AD because greater tolerability and ease of dosing.
    • - CNS: h/a, sleep disturbance, dizziness, anorexia, tremor, nervousness
    • - GI: N, D, C, dry mouth, GI bleeding
    • - sweating
    • - sexual dysfunction
    • - DI: MAOIs, CYP450 inducers, CYP450 inhibitors.
  4. SNRIs for depression
    • venlafaxine, desvenlafaxine, duloxetine
    • - inhibit reuptake 5-HTP, NE, dose dependent.
    • - low doses: SSRI
    • - med doses: + NE block
    • - high doses: + DA block
    • - Use: depression, neuropathic pain, pain ass`d with fibromyalgia
    • - SE: CNS: sleep disturb, insomnia, drowsiness, dizziness, nervousness
    • - GI: nausea, dry mouth (Ach) at high doses
    • - CVS: htn at high doses
  5. NE and DA reuptake inhibitors
    • bupropion
    • - antidepressant effects thru NE and DA reuptake inhib
    • - blockade of DA uptake > NE uptake
    • - sx of DA deficiency targeted: anhedonia, hypersomnia, cognitive slowing, inattention, craving
    • - good sub for SSRI-induced sexual dysfunction
    • - Use: depression, smoking, ADHD
    • - SE: agitation, anorexia, insomnia, Sz (dose dependent)
    • - CI: current Sz disorder, bulimia or anorexia nervosa (GABA changes inc risk of sz)
    • - DI: MAOIs
  6. 5-HT antagonist/reuptake inhibitor
    • trazodone
    • - potent blocker of post-synaptic serotonin receptors
    • - weak serotonin reuptake blocker
    • - Use: depression, hypnotic in depressed pts
    • - SE: daytime sedation at tx doses
    • - orthostatic hypo, N, h/a, priapism, dry mouth
  7. NE and specific 5-HT antidepressants
    • mirtazapine
    • - drug blocks central presyn alpha-2 adrenergic inhibitory autoreceptors
    • - results in increased central NE and 5-HTP activity
    • - Use: depression
    • - SE: antihist (weight gain, sedation), antiadrenergic (orthostatic hypotension)
    • - DI: MAOIs
  8. chronic antidepressant use:
    • - desensitization of of post-synaptic receptors
    • - block NMDA receptors (reduce glutamate activity), increase synthesis of microtubules (change signal transduction), enhance synth and transport of NT synthesizing enzymes (tyrosine and tryptophan hydroxylase)
    • - normalize muscarinic supersensitivity
    • - reduce proinflammatory cytokines and PGE2 (and normalize/increase central MA release)
    • - reduces cortisol, increases BDNF (transcription factor) to increase neuronal plasticity and recovery (esp increase hippocampal volume)
    • - sensitizes GC receptors on catecholamine and 5-HT cell bodies to normalize NE and 5-HT function (that is reduced by hypercortisolemia)

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