Drugs for Movement Disorder _ kruse Flashcards
What receptor does Levodopa bind to?
D2
What is the first line therapy for PD symptoms?
Levodopa
What can be prescribed to reduce peripheral metabolism of levodopa and thus increase half life and better transmission to CNS?
Carbidopa
What CV AE are associated with levodopa?
- postural hypotension
- Hypertension with large dose or with nonselective monoamine oxidase inhibitors or sympathomimetic
- increase cardiac arrhythmias, rare but can happen
What behavioral effects are seen with levodopa use?
- depression, anxiety, agitation, insomnia, somnolence, confusion, delusions, hallucinations, nightmares, euphoria, other changes in mood or personality
Explain the on-off phenomenon as seen with use of levodopa.
Occur due to timing of dose or due to unrealted reason. In on-off, periods of marked akinesia alterante over the course of a few hours with on-periods of improved mobility but often marked dyskinesia.
PD patients taking levodopa, can develop on-off phenomenon. What drug can be given to those with severe case of off-periods?
Apomorphine
What are the contraindications with levodopa?
- pts taking monoamine oxidase A inhibitor –> hypertensive crisis
- Psychotic pts
- pts with angle-closure glucoma
- hx of melanoma
Bromocriptine, pramipexole and ropinirole are all 1 receptor agonist. Indicate what receptor each of them work in
They’re all dopamine receptor agonist used to treat PD symptoms.
Bromocirptine = D2 agonist (also for tx of endocrine disorder)
Pramipexole = D3 (also approved for RLS
Ropinirole = D2 (also approved for RLS)
Bromocriptine is contraindicated in pts with _
peripheral vacular disease
What are the two common MAO inhibitors?
Selegiline and Rasagiline . both inhibit MAO -B
what is the MOA for MAO inhibitors?
slows breakdown of dopamine and prolongs antiparkinsonism effects of levodopa; reduce on-off periods
What drugs are commonly used as COMPT inhibitors?
Tolcapone and entacepone
What is the MOA of COMT inhibitors?
Metabolze levodopa to 3 0-methyldopa, which competes with levodopa for transport across intestinal mucosa and BBB –> prolongs levodopa
Which COMT inhibitor is associated with liver failure and death?
Tolcapone
What is the MOA of apomorphine?
Dopamine agonist that appears to act by stimulating postsynaptic D2 receptor in caudate-putamen. Can in injected subq for quick off period relief.
which drug is presumed to work by enhancing the action of endogenous dopamine and is associated with livedo reticularis, and should be cautioned in pts with seizures and HF
amantidine
Anticholinergic drugs used to treat PD symptoms, helps with which symptoms mainly?
Mainly tremor and rigidity, but have little effect on bradykinesia
What are the common anti-cholinergic drugs used for PD tremor and rigidity?
Benztropine, biperiden, orphenadrine, procyclidine, trihexyphenidyl
Reserpine and tetrabenzaine have been known to impair _
dopamineric neurotransmission of alleivate chorea as seen in HD.
What is the MOA for reeserpine and tetrabenzaine?
Reserpine (irreversible) and tetrabeznaine (reversible) are agents that block vesciular monoamine transporter and deplete cerebral dopamine stores
Botulinin toxin A, a-drenergic agents like clonidine, guanfacine) and neuroleptic antipscyhotics like pimozide all have been known to help relieve symptoms of what movement disorder?
Tics
What drug is the only drug that which can prolong life by a few months and is often used in patients with ALS?
Riluzole
Penicillamine, potassium disulfide, and trientine have been used to treat what disease?
Wilson’s disease
