Parkinson's Meds

Cards (8)

  • What meds are available for Parkinson's Disease
    • Dopamine precursors: Levodopa, Carbidopa, and combo (aka Sinemet)
    • Catechol o methyltransferase: Entacapone
    • Monamine oxidase inhibitors: Rasagiline, Selegiline
    • Antiviral: Amantadine
    • Dopamine agonists: Pramipexole, Ropinirole (Requip), Rotigotine
    • Cholinergic receptor antagonist: Benztropine
  • Dopamine precursors
    Levodopa, Carbidopa aka Sinemet if combo
    • Levodopa is immediate precursor to dopamine and is able to cross the BBB 
    • anorexia, nausea, vomiting, tachycardia, ventricular extrasystoles, hypotension, discoloration of saliva and urine, visual/auditory hallucinations, dyskinesias, depression, psychosis, anxiety
    • contraindicated in closed angle glaucoma, hypersensitivity, concomitant MAOI use, caution in hx of melanoma
  • Dopamine precursor clinical info
    • Interactions with MAOI (hypertensive crisis), Antipsychotic drugs (can block dopamine receptors, clozapine better), vitamin B6 (increase peripheral break down, but not an issue if using combo form) 
    • Absorption is affected by drugs that delay or promote gastric emptying
    • Most clinically effective therapy for PD symptoms, effective for all 3 cardinal symptoms (resting tremor, bradykinesia, rigidity)
  • Catechol-o-methyltransferase: Entacapone
    • inhibit conversion of levodopa to 3-O-methyldopa in periphery and CNS, allowing for higher concentration
    • diarrhea, nausea, anorexia, dyskinesias, hallucinations, sleep disorders, fetal hepatic toxicity (tolcapone)
    • Contraindicated in hypersensitivity
    • May help reduce sx of “wearing off”, may need to decrease levodopa dose to avoid adverse dopaminergic effects
    • NOT useful as monotherapy, only in combo with levodopa
  • Monamine oxidase inhibitors: Rasagiline, Selegiline
    • block oxidative degradation of dopamine through MAO-B inhibition 
    • confusion, dyskinesias, hallucinations, hypotension, insomnia, nausea, HTN crisis
    • Contraindicated with MAOIs, transdermal contraindication w/ SSRIs, SNRIs, tricyclic antidepressants, MAOIs, Meperidine
    • Can be initial therapy or adjunct with levodopa, selegiline has higher incidence of HTN and is metabolized by amphetamine so can lead to insomnia, Rasagiline 5x as potent
    • Theorized to slow disease progression caused by reduced oxidative stress
  • Antiviral: Amantadine
    • An antiviral that increases release of dopamine, blocks cholinergic receptors, inhibits NMDA type of glutamate receptors
    • dry mouth, hypotension, livedo reticularis, nausea, restlessness, sedation, vivid dreams
    • renal dosage adjustment
    • Can be initial monotherapy for mild-moderate disease or adjunct w/ levodopa in advances disease, may improve rigidity and bradykinesia, and may be useful to tx dyskinesias associated with long term dopaminergic treatment
  • Dopamine agonists: Pramipexole, Ropinirole (Requip), Rotigotine
    • directly stimulate dopamine receptors
    • nausea, hallucinations, insomnia, dizziness, constipation, hypotension
    • fewer long term motor complications but less effective, may need to decrease levodopa if taking together, does NOT cause fibrosis or peripheral vasospasm as seen with ergot derivative
    • Rotigotin is transdermal patch to tx early PD, admin once daily
    • Initial or adjunct w/ levodopa, longer duration of action than levodopa (good for pts w/ fluctuations in response to levodopa treatment)
  • Cholinergic receptor antagonists: Benztropine
    • compete with acetylcholine at muscarinic receptors in the CNS
    • mood changes, dry mouth, vision problems, confusion, hallucinations, urinary retention, constipation
    • Contraindicated with glaucoma, prostatic hyperplasia, pyloric stenosis, dementia
    • Less effective than dopaminergic drugs but may be good as adjunct therapy, targets tremor more than other sx