Antiparkinsons Drugs Flashcards
How common is Parkinson’s disease? Which gender is affected more? What’s the ratio?
#2 most common neurodegenerative disease
Men> women
3:2
What is MOA of PD? What percent of neurons die before Sx are seen?
Degeneration of DA neurons in substantial nigra
80%
What causes Parkinson’s? Give example for each?
Genetics
-mutations in several genes
Environment
- toxins
- head injuries
Where does ACh come from in the mid brain?
Striatum
- caudate
- putamen
What does The substantia nigra produce?
DA
What does the basal nuclei/ganglia do for the body?
Plans, organizes and coordinates motor movement
What are the Sx of PD?
TRAP B
Resting tremor Rigidity Akinesia Postural instability Bradykinesia
- speech issues
- swallowing issues
What type of Therapy is used to Tx PD?
Physical therapy Speech therapy Occupational therapy Exercise Medication
Which type of therapy for Tx of PD is the most effective in slow progression of the disease?
Exercise
What is the precursor for dopamine?
L-dopa
What breaks down L-dopa in the periphery?
Dopa-decarboxylase
COMT
What inhibits dopa-decarboxylase?
Carbidopa
What inhibits COMT in periphery? What inhibits COMT in the brain?
Tolcapone(Tasmar)
Entacapone(Comtan)
Tolcapone(Tasmar)
What enzymes break down DA in the brain?
COMT
MAO-B
Why drugs inhibit MOA-B?
Selegiline(Eldepryl)
Rasagiline(Azilect)
Safinamide(Xadago)
What drugs are D2 receptor agonist and are used for RLS?
Pramipexole(mirapex)
Ropinirole(Requip)
Rotigotine(Neupro)
What does increased DA in periphery cause?
N/V
Tachycardia
What 3 things do not cross the BBB?
Carbidopa
Dopamine
Entacapone(Comtan)
What is the on-off phenomenon of PD? What is the wearing off effect?
On-off phenomenon=Sx switching between mobility and immobility
Wearing off effect=over time Sx begin to appear or worsen
If DA levels are too high what occurs? DA levels too low?
Chorea
Dystopias
PD Sx
What is amantadine(Symmetrel)? What Sx does it relieve? What is it’s MOA?
DA modulator
Reduces tremors and muscle rigidity
Increase DA release
Blocks reuptake of DA
Anticholinergic properties
Why isn’t tolcapon(Tasmar) used very often?
B/c it causes liver issues
What ADR can happen with entacapone(comtan)?
Darken urine and sweat
What is added to levodopa/carbidopa to reduce on-off phenomenon?
Entacapone(comtan)
What is bromocriptine(Parlodel)? What does it do?
Dopamine receptor agonist
Decreases PRL
What is and ADR for DA agonists?
Delusions
Hullucinations
What drugs are used for RLS(restless leg syndrome)?
Ropinirole(requip)
Pramipexole(mirapex)
Rotigotine(neupro)
How long of an effect does carbidopa/levodopa medication have on the body?
Medications lasts about 5 years
Why should you not eat a protein containing meal one-half hour before or one hour after taking carbidopa/levodopa?
Because the protein and levodopa compete for the same Amino acid transporter to enter the brain
What are the 5 ADR for carbidopa/levodopa?
N/V Orthostatic hypotension Tachycardia Psychosis Insomnia
What does carbidopa/levodopa cause orthostatic hypotension?
Because L-dopa depresses brain stem
Why does taking carbidopa/levodopa sometimes cause insomnia? How can you prevent insomnia from occurring?
B/c the meds are stimulatory
drugs need to be taken several hours before bed
What is benztropine(cogentin)? What Sx does it reduce? What are the ADR of anticholinergics?
Anticholinergic
Reduces tremors and muscle rigidity
Decreases saliva
Tachycardia
Miosis
What is aphasia?
Difficulty speaking
What is dysphagia?
Difficulty swallowing
What is the central triad of PD?
Bradykinesia
Tremors
Rigidity