Antiparkinson Medications Flashcards
Parkinson disease
Chronic, progressive, neurodegenerative disorder
Affects dopamine-producing neurons in the brain
Parkinson disease is caused by an imbalance of two neurotransmitters?
Their actions?
ACh- excitatory
Dopamine- inhibits nerve actions (inhibitory)
Parkinson disease symptoms
Bradykinesia (slow, movement)
“TRAP”
Tremor
Rigidity- of muscle
Akinesia – no movement
Postural instability
Symptoms occur when about 80% of the dopamine stored in the ________ _____ of the basal ganglia is depleted. (20% left of dopamine- far along the disease before diagnosis)
Symptoms can be partially ________ as long as there are functioning _____ ______that can take up dopamine.
Symptoms occur when about 80% of the dopamine stored in the substantia nigra of the basal ganglia is depleted. (20% left of dopamine- far along the disease before diagnosis)
Symptoms can be partially controlled as long as there are functioning nerve terminals that can take up dopamine.
akinesia
absence of psychomotor activity- masklike facial expression
bradykinesia
slow movement
rigidity
cogwheel rigidity, resistance to passive movement
tremor
pill-rolling- the tremor of the thumb against the forefinger
postural instability
unsteadiness
Dyskinesia
Difficulty in performing voluntary movements
Two common types of Dyskinesia
chorea and dystonia
Chorea
irregular, spasmodic, involuntary movements of the limbs or facial muscles
Dystonia
abnormal muscle tone leading to impaired or abnormal movements
Parkinson disease
Rapid swings in response to levodopa occur. Called?
Parkinson’s disease (PD) worsens when too little ________ is present.
_________ occurs when too much dopamine is present.
Rapid swings in response to levodopa occur (“on–off phenomenon”)
Parkinson’s disease (PD) worsens when too little dopamine is present.
Dyskinesia (problem with movement) occurs when too much dopamine is present.
What is “Wearing-off phenomenon”
the drug is losing effectiveness
“on-off phenomenon”
variable response to levodopa, resulting in periods of good control and periods of poor control of PD symptoms
worsening of symptom near the end of the next dose
swings in the response of levodopa
On phenomenon
greater symptom control
Off phenomenon
less symptom control
PD is thought to be caused by an imbalance of _____ & _____ with a deficiency of _______ in certain areas of the brain.
PD is thought to be caused by an imbalance of dopamine and ACh with a deficiency of dopamine in certain areas of the brain.
Drug therapies are aimed at
at increasing the levels of dopamine or antagonizing(lowering) the effects of ACh.
Unfortunately, current drug therapy does not slow the progression of the disease but rather is used to
slow the progression of symptoms.
What type of drug is given first?
direct acting
Part of brain where dopamine deficit occurs?
substantia nigra
(destruction of substantia nigra by PD)
Dopamine depletion reults in
excessive unopposed ACh (cholinergic activity) due to lack of dopamine effects
diagnostic of PD
Lab tests
based on symptoms
CT/ MRI… to rule out other disease
No lab test to detect or confirm PD
end of dose wearing off
diminishing dopamine effect towards the end of the dose associated with increased loss of stored dopamine
direct-acting dopaminergic drugs- define:
2 subclasses
first-line agents
non dopamine dopamine receptors
dopamine replacement drugs
2 subclasses non dopamine dopamine receptors and give examples of each
ergot derivative (bromocriptine)
non-ergot drugs (pramipexole and ropini-
role).
Levodopa is the
Levodopa is a precursor of dopamine.
Blood–brain barrier does not allow _________ to enter but does allow ________.
Blood–brain barrier does not allow exogenously supplied dopamine to enter but does allow levodopa.
give 1 example of nondopamine dopamine receptor agonists
and its subclass
Ergot derivatives: bromocriptine
direct-acting nondopamine dopamine receptor agonists: mechanism of action
directly stimulate PRE and POST synaptic dopamine RECEPTORS in brain
Bromocriptine indications
Parkinson’s disease
hyperprolactinemia
bromocriptine 1 mechanism of action
activates presynaptic dopamine receptors to stimulate more dopamine production
chief site of activity is D2 subclass of dopamine receptors
bromocriptine other mechanism of action
Also INHIBIT the production of the hormone PROLACTIN, which stimulates normal lactation
Can be used to treat women with excessive or undesired breast milk production (galactorrhea) and for treatment of prolactin-secreting tumours
Bromocriptine contraindications
why?
CAUTION: severe ischemic disease: peripheral vascular disease– due to its ability to stimulate dopamine receptors in peripheral tissues outside brain-vasoconstriction worsens PVD
adrenergic drugs due to cardiovascular risks of excess catecholamine activity
bromocriptine may be used with levodopa to
decrease dose of levodopa
bromocriptine adverse effects
GI upset, dyskinesias, sleep disturbances
bromocriptine interactions
erythromycin
adrenergic drugs (increases hr, bp- vasoconstriction)
1 example of Dopamine replacement drugs
Levodopa
Levodopa is
biological precursor of dopamine required by the brain for dopamine synthesis
exogenous source
Levodopa mechanism of actions
stimulate presynaptic dopamine receptors to increase dopamine in brain