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2011-05-02 20:13:23
anti parkinson

Anti-parkinson Pharm V
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  1. Neurodegenerative disease involving extrapyramidal system (where specifically and e.g.)?!
    • substantia nigra and striatum
    • Hypokinetic (rigid): Parkinsonism
    • Hyperkinetic (choreic): Huntington's; also genetically determined
  2. Neurodegenerative disease involving muscle weakness & atrophy? (e.g. and where?)
    • degenerate motor neurons in spinal cord and cerebral cortex
    • ALS (aka Lou Gehrigs)
  3. Neurodegenerative disease characterized dementia (what it affects and e.g.)?
    • neurons in hippocampus and cerebral cortex
    • Alzheimers
  4. Factors in selective neurodegeneration? (4 main factors)
    • Genetic and environmental interaction: genetic link (huntingtons), environmental toxins or viral
    • Excitotoxicity: excessive glutamate release cause excessive influx of Ca++
    • Energy Metabolism: drug-induced or age associated decline in metabolism; change membrange potentials, remove Mg2+ block of NMDA-receptor activation, increase Ca++
    • Free Radicals: eliminated by superoxide dimutase, glutathione, ascorbate ( can produce DNA, protein damage and lipid peroxidation of membranes)
  5. Characteristics of Parkinson's?
    • bradykinesia
    • tremors (at rest)
    • muscular rigiddity
    • abnormal posture
    • mask-like face and shuffling gait
    • impaired speech
    • inability to perform skilled tasks
  6. Pathology of Parkinson's Disease?
    • degeneration of nigrostriatial dopamine (DA) neurons
    • project to striatum (caudate nucleus and putamen)
    • Lewy bodies (surviving neurons)
  7. Etiology of Parkinson's?
    • idiopathic
    • aging, environmental and genetic
  8. What are Parkinsonism disorders? (4 e.g.)
    • encephalitis lethargica
    • multiple small strokes
    • traumatic brain injury
    • antipsychotic drugs (chlorpromazine and haloperidol)
  9. In the normal physiology of the Basal ganglia, what do D1 receptors control and how?
    • direct pathway
    • DA activates GABA
    • inhibit HABA neurons that project to thalamus
  10. In the normal physiology of the basal ganglia, what do D2 receptors control and how?
    • indirect pathway
    • DA inhibit indirect output
    • activate GABA neurons
    • inhibit Glut neurons
    • decrease GABA neurons that project to thalamus
  11. What happens during abnormal functioning of the basal ganglia after degeneration of Dopaminergic Neurons?
    • Decrease DA acting on D1 and D2
    • inhibit direct
    • activate indirect: activate GABA nruons to the thalamaus
    • inhibit GLUT neurons to cortex
    • net decrease in excitator input ot the cortex
    • disruption of muscle control
  12. What are the drugs that increase DA synthesis?
    • L-DOPA
    • L-DOPA/Carbidopa
    • Entacapone
    • Entacapone/L-DOPA/carbidopa
    • Amantadine
  13. L-DOPA: availability? distribution?Peripheral side effects? CNS side effects?
    • precursor to DA
    • tx: symptoms; rigidity, tremors
    • oral, small intestine
    • "wearing off" effect: 3-5yrs
    • 1-3% reaches brain (huge problem for side effects): peripher effects: n/v, anorexia, cardiac arrythmias, orthostatic hypotension
    • CNS: visual and auditory hallucinations, dyskinesia, mood changes, depression, psychosis
  14. Carbidopa actions and significance?
    • blocks peripheral metabolism of L-DOPA
    • so increase L-DOPA available to brain
    • allows to reduce dose by 4-5 fold
  15. Entacapone MOA?
    inhibitor of catechol-omethyltransferase
  16. What are the drugs that decrease DA catabolism?
    • Selegiline
    • Rasagiline
  17. Selegeline: MOA, availability, metabolized?
    • inhibits monoamine oxidase type B (MAO-B)
    • decrease hydrogen peroxide, limiting free radicals
    • in combo with levodopa (little benefit when alone)
    • oral, renal excrete, half-life:7-9hrs
    • metabolized to methamphetamine and amphetamine (insomnia)
  18. Rasagiline
    • selective inhibitor of BRAIN MAO-B
    • not metabolized to amphetamine
  19. What are the Dopamine receptor Agonists? (4)
    • Bromocriptine: D2 ag + D1 partial ag
    • Ropinirole: D2+D3 ag
    • Pramipexole: D2+D3 ag
    • Apomorphine
  20. Dopamine Receptor Agonists: administration, side effects?
    • monotherapy in early stages
    • oral: low dose and gradual icnrease to therapuetic effect
    • adverse: cardivascular (arrythmias, postural hypotension), neurological (depression, confusion, hallucinations, sleepiness, impulsivity), GI (n/v/),
    • Contra: heart or mental problems!
  21. Apomorphine: use, administration, side-effects?
    • acute tx w/ advanced disease for "off" periods (maked bradikinesia, immobility)
    • subQ (NO IV)
    • side-effects: n/v, arrythmias, postural hypotension, hallucinations, pronounced sleepiness
  22. What are the muscarinic Antagonists: mechanism, side-effects? (2)
    • Benztropine, Trihexyphenidyl
    • alleviate tremor and rigicity (not bradykinesia)
    • MOA: loss of nigrostriatal neurons (inhibit Ach release) leads to increased firingof striatal cholinergic interneurons and overstimulation of muscarinic receptors; these will block this
    • side-effects: antimuscarinic effects: blurred vision, dry mouth, urinary retntion, constipation, aggravation of glaucoma, delirium, psychosis, memory impairment
  23. Amantadine? use, MOA, side-effects?
    • bradykinesia and rigidity, prior to L-DOPA
    • MOA: increase DA release, block cholinergic muscarinic receptors and glutamatergic NMDA receptors
    • Side-effects: hallucinations, confusion, nasea, dizziness, rash of low extremeties
    • contra: CHF and glaucoma
    • developed as antiviral for influenza
  24. Implications to dentistry: Musculature
    • hard to swallow
    • tongue muscles
    • hard to brush teeth/floss
    • movements may complicate procedures
  25. What drug can induce dyskinesia?
  26. what drugs can sensitize to epi-induce arrythmias?
    levodopa and MAO-B inhibitors
  27. What drugs can reduce the elimination of Entacapone?
    antibiotics: ampicillin, erythromycin
  28. What are some side effects of the drugs that may effect oral health or appts?
    • xerostomia
    • nausea and vomiting
    • orthostatic hypotension
  29. hope this was helpful, if there is anything wrong then just e-mail me and I think I can edit it...
    Also, I hope I did this right due to the fact that I never use flashcards!