Neurodegenerative Drugs

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  1. levadopa (L-dopa)
    • increase DA synthesis
    • precursor of dopamine
    • wearing off effect within 3-5 years
    • oral, rapid small intestine absorption, 1-3% reaches the brain
    • short half life - 1-2 hours
    • peripheral side effects: nausea, vomiting, anorexia, arrhythmias, orthostatic hypotension
    • CNS side effects: visual and auditory hallucinations, abnormal involuntary movements (dyskinesia), mood changes
  2. L-DOPA/carbidopa
    • medication of choice for symptomatic treatment of Parkinson's
    • carbidopa is an aromatic l-amino acid decarboxylase inhibitor, blocks metabolism of L-dopa into dopamine peripherally = 4-5 increase in L-DOPA in the brain
  3. entacapone
    catechol-O-methyltransferase (COMT) inhibitor - blocks peripheral metabolism of L-DOPA into methyldopa = increase L-DOPA availability to brain
  4. selegiline
    • inhibits MAO-B
    • decreases production of byproduct hydrogen peroxide = limits formation of neurotoxic free radicals
    • adjunctive treatment in Parkinson's
    • orally active, half life 7-9 hrs, renal excretion
    • metabolized to methamphetamine and amphetamine (insomnia)
  5. rasagiline
    • selective inhibitor of MAO-B (more potent)
    • not metabolized to amphetamine-like substance
  6. Bromocriptine
    • D2 agonist and D1 partial agonist
    • effective as monotherapy early in disease or as an adjunct later in disease
    • adverse effects: cardiovascular effects (arrhythmias, postural hypotension), neurological effects (depression, confusion, hallucinations), GI problems,¬†contraindicated in patients with heart or mental problems
  7. ropinirole and pramipexole
    • D2 and D3 agonist
    • effective as monotherapy early in disease or as an adjunct later in disease
    • adverse effects: cardiovascular effects (arrhythmias, postural hypotension), neurological effects (depression, confusion, hallucinations), GI problems,¬†contraindicated in patients with heart or mental problems
  8. apomorphine
    • dopamine receptor agonist
    • acute treatment of patients with advanced disease or for¬†off periods (bradykinesia, immobility)
    • SQ administration (NOT IV - may lead to thrombus formation and PE)
    • adverse effects: nausea, vomiting, arrhythmias, postural hypotension, hallucinations, pronounced sleepiness
  9. benztropine and trihexyphenidyl
    • muscarinic antagonists
    • used to alleviate tremor and rigidity as monotherapy or with other drugs
    • adverse effects: typical antimuscarinic effects - blurred vision, dry mouth, urinary retention, constipation, aggravation of glaucoma, may also produce delirium, psychosis, memory impairment
  10. amantadine
    • used to alleviate bradykinesia and rigidity (not helpful for tremor) in patients with mild to moderate disease prior to L-DOPA initiation
    • moderately increases DA release, blocks cholinergic muscarinic receptors and glutamatergic NMDA receptors
    • adverse effects: hallucinations and confusion, nausea, dizziness, rash of low extremities; special caution in patients with congestive heart disease and with glaucoma
  11. donepezil, galantamine, ravastigmine, and tacrine
    • AChE inhibitors
    • blocks catabolism of ACh
    • modest improvement in some alzheimers patients, benefits retained for several years
    • good oral bioavailability
    • variable pharmacokinetic and half-life time: donepezil - 70 hrs, galantamine - 7 hrs
    • all metabolized by P450 except rivastigmine (plasma cholinesterase)
    • adverse effects: Tacrine may produce hepatotoxicity; tremors, bradycardia, nausea and vomiting, diarrhea, anorexia
  12. memantine
    • NMDA receptor antagonist (low affinity) - derivative of amantadine
    • protects neurons from Calcium overload that leads to neuronal death
    • improved ADL and cognitive fn
    • benefits additive when given with donepezil
    • adverse effects: dizziness, headache, confusion, agitation, constipation

Card Set Information

Author:
jboi
ID:
323979
Filename:
Neurodegenerative Drugs
Updated:
2016-10-02 21:32:48
Tags:
mohd4 pharmacology neurodegenerative
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Description:
MOHD4 lecture 72
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