Pharmacology of Parkinson's Disease Flashcards
What is Amantidine (symmetrel)?
a drug that facilitates the release of endogenous dopamine
Disorders of _____ may predispose pts to subsequent assault by chemicals in Parkinson’s Disease.
mitochondrial energy pathways
How is dopamine broken down?
dopamine + MAO –> DOPAC + catchol-o-methyl transferase (COMT) –> HVA
Neurotoxins such as the meperidine analog _____ can cause a Parkinson’s-like condition by killing dopamine neurons.
MPTP
Name 3 anticholinergic drugs for Parkinson’s treatment.
- Trihexyphenidyl (Artane)
- Benztropine (Cogentin)
- Diphenhydramine (Benadryl)
Name 2 Catechol-o-methyl transferase inhibitors used to treat Parkinson’s.
- Tolcapone (Tasmar)
- Entacapone (Comtran)
What drug facilitates the release of endogenous dopamine?
Amantidine (symmetrel)
Name some possible environmental causes of Parkinsons.
- well water
- pesticides
- copper and iron exposures
What is Sinemet?
L-DOPA combined with a peripheral decarboxylase inhibitor, carbidopa
Collectively, what kind of drug are the following?
- Tolcapone (Tasmar)
- Entacapone (Comtan)
Catechol-o-methyl transferase inhibitors
Name 5 dopamine receptor agonist drugs.
- Bromocriptine (Parlodel)
- Pergolide (Permax)
- Pramipexole (Mirapex)
- Ropinirole (Requip)
- Cabergoline (Dostinex)
Why are anticholinergic drugs used for Parkinson’s therapy? How effective are they? Why aren’t they used as often?
to treat the tremor; less effective than L-DOPA; anti-parasympathetic side effects
Name 2 MAOIs used to treat Parkinson’s.
- Selegiline, also called Deprenyl - (Eldepryl)
- Rasagiline (Azilect)
What is the significance of alpha-synuclein?
- it’s a mutated protein in the auto. dominant form of Parkinson’s
- is also found in the Lewy bodies in Parkinson’s patients w/o the mutation
Why do some neurologists choose to start with a dopamine agonist, rather than L-DOPA?
there’s less risk of dyskinesia
These drugs prevent the breakdown of L-DOPA and dopamine by COMT.
catchol-o-methyl transferase (COMT) inhibitors
How is L-DOPA administered? How does it reach its target?
orally; crosses the BBB
The first mutation found assoc. with Parkinson’s is a single aa change in the protein, ______.
alpha-synuclein
Collectively, what kind of drug are the following:
- Bromocriptine (Parlodel)
- Pergolide (Permax)
- Pramipexole (Mirapex)
- Ropinirole (Requip)
- Cabergoline (Dostinex)
dopamine receptor agonists
Drug-induced Parkinsonism is a common side effect of _____ and other _____ drugs.
phenothiazines; neuroleptic
What is the most important drug for Parkinson’s tx?
L-DOPA
What seems to be the common physiological pathway in the pathology of Parkinson’s disease?
- destruction of dopamine cells in the pars compacta of the substantia nigra
- loss of the NT dopamine in the caudate and putamen
How do catchol-o-methyl transferase (COMT) inhibitors work?
prevent the breakdown of L-DOPA and dopamine by COMT
______ inhibits liver enzymes and has caused liver toxicity.
Tolcapone
Tolcapone inhibits _____ enzymes and has caused _____ toxicity.
liver x2
What are the cardinal features of Parkinson’s Disease?
- tremor
- rigidity
- akinesia
This is a drug that blocks decarboxylase in the intestines and peripheral organs but does not cross the BBB.
carbidopa
What is carbidopa?
a drug that blocks decarboxylase (and levodopa breakdown) in the intestines and peripheral organs but does not cross the BBB
These drugs directly stimulate the dopamine receptors in the caudate/putamen.
dopamine receptor agonists
Collectively, what kind of drug are the following?
- Selegiline, also called Deprenyl - (Eldepryl)
- Rasagiline (Azilect)
they’re MAOIs used to treat Parkinson’s
What do dopamine receptor agonists do?
directly stimulate the dopamine receptors in the caudate/putamen
Collectively, what kind of drug are the following?
- Trihexyphenidyl (Artane)
- Benztropine (Cogentin)
- Diphenhydramine (Benadryl)
they’re anticholinergics used to treat Parkinson’s
How is dopamine synthesized?
tyrosine + tyrosine hydroxylase –> L-dopa + DDC –> dopamine
Which receptor do most of the dopamine receptor agonists work at?
the dopamine D2 receptor
How do MAOIs help Parkinson’s disease?
they prevent the breakdown of dopamine