sem 2 pharm 1

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sweetlu
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sem 2 pharm 1
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2012-02-19 09:46:33
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sem 2 pharm 1
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  1. Neurogenesis in adults can occur here
    • - dentate gyrus of the hippocampus
    • - olfactory bulb
  2. Opiods
    • - centrally acting analgesics
    • - mu agonist (work on same receptor as endorphins)
    • - work on ascending and descending pain tracts
    • -(down) DISinhibit GABAs inhib. actions on Ser and NE
    • - (up) block NT release from presyn. via blocking Ca channels and hyperpolarize postsyn. via opening K channels
    • - Morphine- full mu agonist, full efficacy
  3. epicritic pain
    - easily discriminable and well localized
  4. protopathic pain
    - not localized and can only be described generally
  5. ASA
    • - irreversible COX inhibitor
    • - anti-inflammatory, fever, pain, and thrombotic effects
    • -**increased risk of bleeding**
  6. NSAIDS
    • - reversible COX inhibitors
    • - inhibit pain and inflammation
  7. APAP
    • - COX inhibitor in spinal cord and brain
    • - reduces pain and fever
    • - NO effect on inflammation
  8. When is combonation therapy ok
    - when MOA of the drugs is different
  9. Steroids
    - prevent inflammatory mediator production by working on hormone receptors
  10. Local anesthetics
    • - block neuronal firing
    • - effective against nociceptive and neuropathic pain
  11. local analgesics
    • - nociceptive and neuropathic pain
    • - Lidocaine- Na channel blocker- slow rapid firing of voltage gated Na ion channels
    • -Capsacin- substance P- stimulates C fibers- overstimulation causes temporary nerve ending damage, reducing ability to send pain signals
  12. enkephalins
    • - act on delta receptors for distraction of pain
    • - Nucleus Raphe Magnus will stimulate the release of enkephalins(via seratonin) from inhibitory neurons in spinomesencephalic tract after pain signal reaches PAG via
  13. NMDA-r antagonist
    • - block Ca influx
    • - Ketamine- serious side effects like dysphoria and hallucinations
  14. Catecholamine synthesis
    L-tyrosine--(tyrosine hydroxylase** + BioH4)--> L-DOPA

    L-DOPA--(DOPA decarboxylase+B6)--> DA

    DA--(Cu+ Vit C)--> NE--(SAM)--> Epi

    **= irreversible regulatory step
  15. Inactivation of catecholamines and indoleamines
    • -taken back up into nerve by high affinity uptake Na cotransport**
    • 1. MOA- oxidative deamination
    • 2. COMT- methylation
    • **= transporter is rate limiting step
  16. Indoleamine synthesis
    • L-Trp--(Trp hydroxylase+BioH4)--> 5-OH-Trp
    • 5-OH-Trp--(decarboxylase+B6)-->5-HT(seratonin)
  17. MAOIs
    • - can cause HTN when exposed to foods containing tyamine(cheese and redwine)
    • - MAO-A for 5-HT(seratonin)
    • - MAO-B for DA
  18. amitryptiline
    • - tricyclic antidepressant
    • - inhibit high-affinity uptake of NE and 5-HT(seratonin)
    • - approved for use in neuropathic pain
    • - side effect- anticholinergic effects
    • - not for patients over 65
  19. SSRI
    - inhibit uptake of 5-HT only
  20. cocaine and methylphenidate
    -inhibit uptake of DA,NE and 5-HT
  21. amphetamine
    - releases DA and 5HT from nerve terminals
  22. Barbituates
    • stimulate GABA-A receptor
    • - cause increase in Cl conductance
    • - hyperpolarize
  23. Benzodiazepines
    • - sensitize GABA-A receptor
    • ** no suicide risk**
    • - increase Cl conductance
    • - hyperpolarize
  24. duloxetine
    • - SNRI (seratonin, NE reuptake inhibitor
    • - approved for peripheral diabetic neuropathy
  25. gabapentin and pregabalin
    • - anticonvulsant
    • - blocks Ca influx by binding to alpha 2 delta s/u of Ca ion channel
    • - blocks release of glutamate and substance P
  26. Thalamic pain syndrome
    - lesions to posterior thalamus may cause chronic pain
  27. methylphenidate
    • - binds to DAT
    • - reduces rate of uptake and increases extracellular DA
    • - cocaine works this way
  28. Mixed amphetamine salts
    • - triggers phosphorylation of DAT causing reversal of DA and subsequent increase
    • - inhibits uptake and increases release of DA
  29. Dx for inattention
    • - 6 or more for 6 months
    • -often loses thing, creless mistakes, difficulty sustaining attention, poor listener, forgetful, easily distracted, etc
  30. Dx for hyperactivity
    • - 6 or more for 6 months
    • - fidgety, cant remain seated, runs about, etc
  31. dorsal anterior cinculate cortex (dorsal ACC)
    -regulates selective attention
  32. dorsolateral prefrontal cortex
    - sustained attention
  33. prefrontal motor cortex
    - involved in hyperactive sx
  34. orbital frontal cortex
    - involved in impulsive sx
  35. NE in ADD
    • - modulates attention processes through arousal networks in the prefrontal cortex
    • - also important in behavioral inhibition
  36. haloperidol
    -D2 receptor antagonist
  37. COMT
    • - ez involved in DA metabolism
    • -polymorhic (val/met) substitution at gene level increases activity
    • - more activity--> less DA
  38. Seratonin
    • -synth in rapha nuclei
    • - involved in mood, sleep and psychosis
    • - can act as excitatory or inhibitory
    • - ionotropic or metabotropic
    • - therapy target for migraines, anxiety, depression and OCD
  39. Fluoxtine
    • -Seratonin Reuptake Ihnibitor (Ser/Na cotrans inhib)
    • - can be used to heal (temporary tx)
  40. ACh
    • - ligand and metabotropic receptors
    • - receptors in basal ganglia, cortex and hippocampus
    • -loss of central muscarinic cholinergic neurons-> AD
  41. diphenhydramine
    • -histamine blocker
    • - not for pt over 65-> can cause delirium
  42. NE
    • - made in locus coeruleus in pons
    • - function- arousal, sleep/wake cycle, pain, inflammation, emotions, learning and memory
  43. Clonidine
    • - dampens NE tone
    • - used in opiate withdrawl
    • - can be used in tx of ADD, ax, depresson
  44. GABA
    • A- ionotropic receptor, increase Cl conductance
    • B- metabotropic receptor, increase K conductance

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