antidepressants

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thedewhub
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301090
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antidepressants
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2015-04-19 16:48:28
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antidepressants
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antidepressants
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antidepressants
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  1. length of time AD take to work
    3 or more weeks
  2. factor associated with neural plasticity, resilience, and neurogenesis
    brain derived neurotrophic factor
  3. effective AD therapy do this
    increase neurogenesis ans synaptic connectivity by increasing BDNF
  4. AD drugs increase levels of
    NE, 5HT, and dopamine which act to increase BDNF levels, promotes development of new connections in limbic, cortical, and hippocampal circuitry
  5. Antidepressant Drugs increase
    • the amount of NE and/or 5HT at cortical and
    • limbic synapses.
  6. Tricyclic Antidepressants (TCAs) block
    the reuptake of NE and (to a lesser extent) 5HT into nerve terminals by blocking the transporter at presynaptic terminals (NET, SERT). They also block alpha 1 receptors.
  7. MAO Inhibitors (MAOIs) block
    the metabolic breakdown of NE and 5HT.
  8. Selective Serotonin Reuptake Inhibitors (SSRIs)
    block the reuptake of 5HT and (to a lesser extent) NE into nerve terminals by blocking the transporter at presynaptic terminals (NET, SERT).
  9. Selective Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs)
    • block the reuptake of both NE and 5HT into nerve
    • terminals by blocking the transporter at presynaptic terminals (NET, SERT).
  10. TCA AE
    anti-muscarinic, antihistaminic, and alpha 1 receptor -blocking actions
  11. fluoxetine stuff and SE
    • SSRI, geriatric and ped depression, bulemial PMDD, OCD
    • metabolized into norfluoxetine- more active 3x
    • AE- HA sweating, anxiety agitation, GI, weakness and fatique and sexual dysfn, weight and sleep changes. Numerous drug rxn CYP2d6 especially with TCA, neuroleptics, cardiac and BB drugs
  12. sertraline
    • SSRI
    • less rxn than fluoxetine. adult depression, OCD in 6yo, panic d/o, PTSD, social phobia, PMDD, schizo depression, brain injury beahvioral probs, premature ejac.
  13. most delayed onset of effects of SSRIs
    • sertraline
    • Highly protein bound, 1 week to establish Css,
  14. citalopram
    • SSRI
    • weak inhibitor of CYP2D6 less likely to inhibit metabolism. NOT approved for children or depression. effective in reducing hot flashes in menopause
  15. escitalopram
  16. SSRI, s enatomer of citalopram- no evidence that SE profile is less than racemic. Used for GAD- generalized anxiety d/o. and adolescent depression
  17. SSRI generalized AE
    • mainly because of increased Serotonin levels, NVD, GI, usually emerge early and cease in first week.
    • DISCONTINUATION syndrome- after abrupt WD,
  18. agents at high risk for discontinuation syndrome
    • short half lives and inactive metabolites like citalopram and escitalopram.
    • fluoxetine has lowest DS risk
  19. S/Sx of discontinuation syndrome
    HA, malaise flu like sx, agitation, irritability, nervousness, and sleep changes
  20. Serotonin syndrome
    rare but dangerous elevation of 5HT- hyperthemia, muscle rigidity, myoclonus, rapid fluctuation in mental status and VS. liklihood increases with concurrent SSRI use
  21. all SSRi can do this to depression
    transform it into mania- should be stopped if develops, and mania therapy should be initiated
  22. venlafaxine/ desvenlafaxine
    SNRI, dual inhibitors of both serotonin and norepi and is effective in treating pts with melancholia- severe form of depression. minimal protein binding conferring good bioavail, PTSD, PMDD, hot flashes in Ca
  23. SE of venlafaxine/ desvenlafaxine
    very similar to SSRIs, nausea constip, insomnia, HA, sedation and sex dysfn.
  24. trmt for women who want to avoid estrogen therapy for menopause
    desvenlafaxine
  25. duloxetine
    • SNRI- well absorbed and good half life, tightly protein bound-- extensive oxidative metabolism
    • GAD, mngt of fibromyalgia, chronic musculoskeletal pain- from OA or other
  26. Atypical AD
    • buproprion,
    • nefazadone
    • trazadone
  27. buproprion
    well tolerated w/ orthostatics w/ TCAs. greater seizure potential. does slightly inhibit dop reupake
  28. nefazadone/trazadone and SE
    • weak 5ht reuptake inhibitors, no anticholinergic or cardiotoxicity
    • SE- Nef associated with hepatotoxicity
  29. MAOI general
    block the metabolism of NE, Dop, and 5ht that may leak out of symnaptic besicles when cell is at rest
  30. major MAOI
    • phenelzine
    • tranycypromine
    • each inhibit MAO irreversably
  31. tranylcypromine
    • MAOI
    • amphetamine like stimulant may produce agitation and insomnia
  32. phenelzine
    • MAOI
    • certain forms of mild bipolar illness
  33. MAOI AE and contra
    • very toxic and unpredictable drug food interactions
    • tyramine in certain foods such as cheese, meats, red wines. with MAOI get rapid release of catcholamines- occiptal HA, stiff neck. htn, tach, nausea, seizures, CVA. strict dietary restrictions.
    • interact with SSRI- serotonin syndrome and buproprion-seizures
  34. TCAs mech and SE
    • NE reuptake block and some Sero. many AE
    • alpha adrenergic, muscarinic, and H1 hist, narrow TI
    • imipramine 5-6 dose is fatal, OR and QT prolong, muscarinic blockade - similar to atropine, ortho hypotndizziness, reflux tach, drowsiness.
    • caution with use in old and young- may have poor compliance
  35. bipolar dz trmt
    AD meds can precipitate mania w/ MDD pts, could be related to epilepsy overrxtive brain. Anticonvulsants seem to have efficacy in trmt of mania- carbamazepine, valproate, lamotrigine, lithium has claming effect
  36. mood stabalizers
    lithium and valproate
  37. most useful trmt for bipolar
    lithium and lamotrigine
  38. useful for aggresion in elderly dementia
    carbamazepine
  39. useful for irritability and impulsivity
    valproate
  40. carbmazepine indi and SE
    • elderly dementia
    • skin rxn, hemat, vc, and liver
  41. valproate indi rxn
    • anticonvulsant for bipolar- agitation and aggresion in dementia- off label
    • nv, thrombocytopenia abnormal coags, increased risk of suicide
  42. lamotrigine indi and SE
    long term maintenance of bipolar I, not for acute mania, risk of steven johnsons syndrome if not titrated- skin and mucous severe rxn- some suicidal ideation
  43. lithium indi and SE
    • manic-depressive- effective in 60-80% of mania, may involve phosphatidyl inositol PW
    • AE- HA, dry mouth, polydipsia, polyuria, GI distress, tremor, fatigue, derm rxn, sedation, ataxia, slurred speech confusion convulsion, decrease thyorid fn. VERY LOW TI
  44. TCAs list
    • imipramine- prototypical
    • desipramine,
    • amitriptyline
    • protriptyline
    • doxepin

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