Pharmacology Exam 4

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Rx2013
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49284
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Pharmacology Exam 4
Updated:
2010-11-13 15:12:26
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Treatment PD other neurodegenerative diseases
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Treatment for PD and other neurodegenerative diseases
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  1. Two types of PD
    • idiopathic
    • drug induced
  2. Idiopathic PD
    • progressive neurodegenerative disorder
    • loss of dopaminergic neurons in the substantia nigra
    • lewy bodies
  3. Drug-induced PD
    • DA receptor antagonists
    • haloperidol
    • thorazine
    • prochlorperazine
    • metoclopramide
    • MPTP
  4. 3 symptoms of PD
    • bradykinesia or akinesia
    • resting tremor
    • muscular rigidity or hypertonicity
  5. Mechanisms to treat PD
    • replacement therapy with dopamine
    • decrease cholinergic neurotransmissions
  6. Anticholinergic anti PD drugs
    • muscarinic acetylcholine receptor antagonsits
    • Trihexyphenidyl
    • Benztropine
  7. Therapeutic application of muscarinic acetylcholine receptor antagonists
    • mild idiopathic PD
    • use with L-dopa for severe idiopathic PD
    • use for drug induced PD
  8. Side effects of Anticholinergic anti PD drugs
    • drowsiness
    • mental slowness
    • tachycardia
    • dry mouth
    • constipation
  9. Contraindications to anticholinergic anti PD drugs
    • prostatic hyperplasia
    • obstructive GI disease
    • angle closure glaucoma
  10. Biosynthesis pathway for DA
    tyrosine =(tyrosine hydroxylase)=> DOPA =(decarboxylase)=> dopamine
  11. Mechanism of action of L-Dopa
    L-DOPA is converted to DA in the basal ganglia
  12. 4 issues after long treatment with L-DOPA
    • diminished effectiveness (3-4 years)
    • levodopa dose not stop the progression of PD
    • Wearing off and end of dose akinesia
    • on/off phenomenon
  13. Side effects of anti PD drugs
    • stimulation of emetic center
    • tachycardia and orthostatic hypotension
    • dyskinesia 80% of pt
    • behavioral agitation or delirium
    • hormonal problems (DA stops prolactin)
  14. Interaction of anti PD drugs with pyridoxine
    amino acid decarboxylase cofactor
  15. Interaction of anti PD drugs with MAOIs
    hypertensive crisis
  16. Interactions of anti-PD drugs with antipsychotics
    Levodopa prohibited in psychotic patients
  17. Drug interactions of anti-PD agents with physostigmine
    cholinesterase inhibitor used for glaucoma
  18. Carbidopa
    • peripheral decarboxylase inhibitor
    • decreases DA in peripheral circulation by conversion of levodopa
    • reduces requirement of levodopa by 75%
    • do not use in antipsychotic induced PD
  19. DA receptor agonists
    • Bromocriptine D2
    • Perglide D1 and D2
    • Ropinirole D2
    • Pramipexole D3
    • Rotigotine (patch)
  20. Levodopa bioavailability
    1-3% passes through BBB
  21. Bioavailability of Levodopa with Carbidopa
    • carbidopa inhibits degredation in the periphery
    • 10% available to cross BBB
  22. Applications for other DA receptor agonists
    • better for on/off phenomenon
    • useful for those who cannot tolerate side effects
    • similar GI and cardiovascular toxicities as L-DOPA
    • contraindicated in psychotic illness or recent MI ro GI ulcer
  23. Amantadine
    • decreases DA reuptake, increases DA release
    • anticholinergic effects
    • antiviral compound
    • use with caution in pt with renal failure, CHF and seizures
  24. Selegiline
    • MAOI
    • irreversible
    • decreases "wearing off" of L-DOPA
    • delays initiation of L-DOPA therapy for PD treatment
  25. Entacapone
    • short duration
    • peripheral COMT inhibitor
  26. Tolcapone
    • long duration
    • actis in CNS and periphery
    • COMT inhibitor
    • 2% hepatotoxicity
  27. Stalevo
    • carbidopa
    • levodopa
    • entacapone
  28. Surgical procedures for anti PD
    • deep brainstem stimulator
    • tissue transplant
  29. Block mACH receptor
    • trihexyphenidyl
    • benztropine
    • amantadine
  30. stimulate D2 receptors on the post synaptic neuron
    • ropinirole
    • bromocriptine
    • pergolide
  31. Neurodegenerative diseases
    • PD
    • Huntingtons Disease
    • alzheimer's disease
    • ALS (amyotrophic lateral sclerosis) (lou gherig's)
  32. PD and Huntington's disease
    loss of neurons in the basal ganglia and abnormalities in control of movement
  33. Alzheimer's disease
    • loss of hippocampal and cortical neurons
    • imparement of memory and cognitive ability
  34. ALS
    • degeneration of spinal, bulbar and cortical motor neurons
    • muscular weakness
    • speak, swallow and facial expression
  35. Factors for Neurodegenterative disorders
    • genetic
    • environmental
    • excitotoxicity
    • oxidative stress
  36. Function of Drugs for AD
    augment cholinergic function in the brain
  37. Cholinesterase inhibitors used for AD
    • tacrine
    • donepezil
    • rivastigmine
    • galantamine
  38. NMDA antagonist used to treat AD
    memantine
  39. Mechanism of drugs for ALS
    • inhibit glutamate release
    • block glutamate receptors
    • relieves spasticity
  40. Drugs for ALS
    • GABAb agonists : Baclofen
    • A2 adrenergic agonists: tizanidine
  41. Tardive dyskinesia
    caused by DA receptor blocker
  42. Tardive dystonia
    da receptor blocker or anticholinergic drugs
  43. tardive akathisia
    anticholinergic anti PD
  44. restless leg syndrome
    • pramipexole
    • ropinirole

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