Anti-Parkinsonism Drugs Flashcards
parkinson is a progressive or nonprogressive disease
progressive
cardinal signs of PD
- bradykinesia or akinesia
- tremors
- muscle rigdity
- postural imbalance
use of dopamine
as a NT in the brain for normal functioning of the extrapyramidal motor system (voluntary movement, balance)
pathophysiology of PD
reduction in Dopamine
pathological hallmarks of PD
- reduction in DA neurons in substantia niagra pars compacta
- inclusion of lewy bodies
NT levels in PD
- reduction in dopamine
- increase in ACh
aim of drug treatment in PD
- give drugs that increase DA levels
- give drugs that decrease ACh levels
anti PD drugs classification
-
dopamine agonists
- bromocriptine
- ropinirole
- pergolide
- pramipexole -
Ach antagonists
- benztropine -
MAO - B Inhibitors
- selegiline
- rasagiline -
COMT Inhibitors
-entacapone
- tolcapone -
sympathomimetics
- adrenaline - dopmaine precursor (L-DOPA)
Adverse effects of L-dopa
LEVODOPA
- lethargy
- excessive sleepiness, euphoria
- vomitting
- orthostatic hypotension
- delirium, delusion
- on and off phenomenon
- psychosis
- athetosis
contraindications of L-dopa
P^G^S^
- peptic ulcer disease
- psychosis
- glaucoma
- gout
- skin lesions
- severe cvs disease like hypotension and arrythmias
drug interactions of L-dopa
- Anti-psychotics
- decrease the effect of l-dopa as they are DA-antagonits - Pyroxidine
- increases L-dopa metabolism, so decreases its effect - MAO inhibitors
- cause hypertensive effect due to increased levels of catecholamines - sympathomimetics
- decrease absorption of L-dope from GIT - anti-cholinergic drugs
- decrease absorption of L-dope from GIT
L-dopa used in combination with
carbidopa
benefits of CT with carbidopa
- increased half life of L-dopa
- decreased dose needed
- reduced adverse effects
ergot derived dopamine agonists
- bromocriptine
- pergolide
non-ergot derived dopamine agonists
- ropinirole
- pramipexole
adverse effects of ergot derived DA agonists
- cardiac valvulopathy
- pericardia, pulmonary, retroperitoneal fibrotic reactions
advantages of dopamine agonists
- can be given in patients who dont have the capacity to convert L-dope to dopamine anymore
- do not require enzymatic conversion to active metabolie
- no toxic metabolites
- no competition for active trasport across bbb
- cause less dyskinesias
advantage of CT of L-dopa
reduction in wearing phenomenon
side effects of dopamine agonists
- fatigue
- somnolence
- nausea
- orthostatic hypotension
- hallucinations
- confusion
contraindications of dopamine agonists
- peptic ulcer disease
- psychosis
- peripheral vascular disease
does ldopa or DA agonist cause more dyskinesia?
l-dopa
is monotherapy of comt inhibitors allowed
NO
one anti-parkinson drug that does not have monotherapy
comt inhibitors
orange discoloraton of urine is a side effect of whic anti-PD drug
comt inhibitors
is monotherapy of mao inhibitors possible
YES
what is a specific side effect of selegiline
production of **amphetamine metabolites **
- nausea
- confusion
- nightmares
- vivid dreams
- hallucinations
- postural hypotension
which mao inhibitor prodcuces amphetamine metabolites
selegiline
which anti-pd drug shows initial flu-like symptoms
rasagiline
one specific side effect of rasagiline
flu-like symptoms
mechanism of action of amantidine
blocks NMDA glutamate receptors and is anticholinergic
whic anti-PD is used as** initial therapy for mild PD**
amantidine
side effects of anti-choliergic drugs
- dry mouth
- blurred vision
- urine retention
- constipation
anti-cholinergic drugs in treatment of pd
- benztropine (cogentin)
- trihexyphenidyl
- orphenadrine
main therpeutic effect produced by anti-cholinergic in pd
reduction of tremors and rigidity but not bradykinesia