pharm stroke and spasticity

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pharm stroke and spasticity
2013-12-19 18:05:44

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  1. glutamate antagonists do what?
    block glutamate receptors to attenuate the neuronal damage caused by anoxia

    CPP, AP-5, AP-7, PCP, MK-801
  2. clot dissolving drug - name?
    tissue plasminogen activator (TPA)
  3. tissue plasminogen activator does what?
    • dissolves clots
    • good bc 80% of strokes are 2/2 blood clots
  4. when should tissue plasminogen activator be given?
    asap, or within 3 hours of onset
  5. Ca++ channel blocking drugs - block what type of channel, and this leads to what? treats what?
    treats stroke: block L-type channels so calcium can't enter the vascular smooth muscle --> less actin-myosin interaction --> vasodilation

    (these drugs aren't as effective on T and N-type calcium channels)

    • diltiazem and nifedipine treat angina and stroke bc by decreasing Ca++ they decrease contraction and O2 demand and alter conduction of electricity
    • dantrolene limits spasticity by reducing muscle contraction
    • verapamil and digitalis treat supraventricular arrhythmia
    • decrease BP (no drug name)
  6. diltiazem - type of drug? effect?
    • a calcium channel blocker
    • vasodilate coronary and periph vessels
    • depresses electrical conduction in SA AV nodes --> bradycardia
  7. nifedipine - type of drug? use in stroke?
    • calcium channel blocker
    • dilate coronary and periph vessels w/o affecting heart excitability/contractibility (they don't impact cardiac striated muscle)

    also used in angina

    part of dihydropyridine class
  8. PAF antagonists - do what 2 things?
    • decrease levels of arachidonic acid
    • postpone neuron death
  9. why too much calcium, glutamate, or arachidonic acid are bad
    Excessive Ca++ from the glutamate cascade will activate enzymes that degrade phospholipids, --> to arachidonic acid, which when metabolized gives rise to oxygen free radicals that destroy cell membranes
  10. mamantene
    • Manages Ca flow through NMDA receptor, but narrow therapeutic window and can kill you
    • so not used.
  11. baclofen - acts where? does what?
    • spinal cord
    • inhibits release of excitatory neurotransmitters
  12. baclofen dosing
    5mg 3x/day up to 80 mg/day
  13. baclofen side effects
    lethargy, weakness, nausea, paraesthesias, SZ w sudden withdrawal
  14. diazepam - drug type, why it helps in spasticity
    • benzodiazepine
    • it's GABA agonistic, mostly at spinal cord --> inhibitory
  15. diazepam doses
    2 mg 3x/day, increasing until effective
  16. side effects of diazepam
    sedation, dependence, cognitive impairment
  17. dantrolene - for what? what does it do basically?
    • spasticity
    • muscle relaxant
  18. dantrolene works where?
    prevents Ca++ release at sarcoplasmic reticulum 

    (baclofen and diazepam operate at the spinal cord)
  19. dantrolene dosing
    • 25 mg/day, then do it 2x/day, 3x, etc
    • if not effective in 45 days, stop
  20. dantrolene side effects
    hepatotoxicity, sedation, weakness, dizzy, paresthesia, nausea, diarrhea

    doesn't cause fatigue bc it works at muscle, not at CNS
  21. clonidine used how?
    in combo with other anti-spasticity drugs (lets you reduce the dose of another drug)

    it reduces symp outflow
  22. clonidine side effects
    • HoTN
    • depression
  23. 2 GABA agonists that limit spasticity
    • baclofen 
    • diazepam

    GABA = gamma-aminobuteric acid
  24. tizanidine (zanaflex) - for what? how?
    • spasiticity
    • Stimulate presynaptic polysynaptic inhibitory pathways.
    • 1/10-1/50th the potency of Clonidine in lowering BP (approved for SC and MS)

    dose 4-36 mg/day
  25. tizanidine - side effects?
    dry mouth, sleepy, asthenia (weakness), dizzy, increased spasm or tone
  26. motor point blocks
    • directed at NMJ
    • used less than motor nerve blocks bc too many injections would be necessary for big muscles
    • treats spasticity
  27. nerve block for spasticity
    directed at the notor nerve, while motor point blocks are directed at the NMJ
  28. what's used to do a therapeutic nerve block?
    first, an anesthetic agent. If it works, more permanenet motor point or nerv blocks can be performed with phenol and alcohol solution
  29. botulinum toxin type A = botox
    treats spasticity how?
    • injection into muscle
    • binds to presynaptic cholinergic nerve terminals inhibiting exocytosis of acetylcholine into NMJ
  30. timing of nerve block and botox effects?
    • blocks - immediate
    • botox - in a few days - lasts months
  31. surgery for spasticity
    • selective dorsal rhizotomy for CP to sever the abnormal dorsal rootlet
    • intrathecal baclofen pump
  32. anesthetic agent used for nerve block
    bupivacain hydrochloride (lasts a few hours)
  33. diazepam vs diltiazem
    • diazepam: GABA agonist - used in spasticity and SZ
    • diltiazem: Ca++ blocker - dilates coronary and periph vessels - used in angina and stroke
  34. 2 antihypertensive / alpha 2 adrenergic agonist drugs to treat spasticity
    • clonidine (catapres)
    • tizanidine (zanaflex)