NCM 235

Antiparkinsonian
Drugs
Parkinson’s Disease:
• Disease of the basal ganglia & related
neuronal groups + neurotransmitter
deficiencies
• “shaking palsy”
Bradykinesia – slowing down in the
initiation & execution of movement
Rigidity – increased muscle tone
Tremor at rest
Impaired postural reflexes
 Parkinson’s Disease
• Degeneration of dopamine-producing neurons in the
substantia nigra of the midbrain
• Symptoms do not occur until 80% of the neurons in
the substantia nigra are lost
• Disrupts the balance of:
 dopamine (DA) – neurotransmitter for normal
functioning of the extrapyramidal motor system
(control of posture, support, and voluntary
motion)
 Acetylcholine (Ach) and the basal ganglia
 Five Stages
1. Flexion of affected arm - tremor / leaning toward
unaffected side
2. Slow shuffling gait
3. Increased difficulty walking – looks for support
to prevent falls
4. Further progression of weakness – assistance
with ambulation
5. Profound disability – may be confined to
wheelchair
 Tremor
• First sign
• Affects handwriting – trailing off at ends of
words
• More prominent at rest
• Aggravated by emotional stress or
increased concentration
• “Pill rolling” – rotary motion of thumb and
forefinger
 Rigidity
• Increased resistance to passive motion when
limbs are moved through their range of motion
“Cogwheel rigidity” -- jerky quality –
intermittent catches of movement
• Caused by sustained muscle contraction
 Muscle soreness; feeling tired & achy
 Slowness of movement due to inhibition of
alternating muscle group contraction &
relaxation in opposing muscle groups
 Bradykinesia
• Loss of automatic movements:
 Blinking of eyes, swinging of arms while
walking, swallowing of saliva, self-
expression with facial and hand movements,
lack of spontaneous activity, lack of postural
adjustment
 Results in: stooped posture, masked face,
drooling of saliva, shuffling gait (festination);
difficulty initiating movement
Masked Face
 Drug Therapy
Correcting the imbalance of neurotransmitters
within the CNS
• Dopaminergic – enhance release or supply
of dopamine (DA)
• Anticholinergic – antagonize or block the
effects of overactive cholinergic neurons in
the striatum
Treating Parkinsonism with Dopaminergic Drugs:
• Increases dopamine levels in the corpus
striatum of the brain
• Drug of choice is Levodopa, which is a
precursor of dopamine synthesis
 Dopaminergic Drugs
1. carbidopa-levodopa (Sinemet) – mainstay in
the treatment of PD
2. amantadine (Symmetrel)
3. apomorphine (Apokyn)
4. bromocriptine (Parlodel)
5. pramipexole (Mirapex)
6. ropinirole (Requip)
 Drug-Drug Interaction
• If dopaminergics are combined with monoamine
oxidase inhibitors (MAOIs), therapeutic effects
increase and a risk of hypertensive crisis exists.
The MAOI should be stopped 14 days before
beginning therapy with a dopaminergic.
• Combination of levodopa with vitamin B6 or with
phenytoin may lead to decreased efficacy of the
levodopa
 Client Teaching
1. Increase fiber and fluid intake to prevent
constipation.
2. Avoid foods high in pyridoxine (vitamin B6) such
as beef, liver, ham, pork, egg yolks, sweet
potatoes, and oatmeal because they will
decrease the effects of the medications.
3. Avoid all OTC drugs and fortified cereals
because of the possible presence of pyridoxine.
4. Immediately report muscle spasm, spasmodic
winking, and an increase in bradykinesia.
5. It may be several months before the full
therapeutic effects is achieved.
A second approach to changing the balance of
between dopamine and acetylcholine in the brain
is to give cholinergic blockers or anticholinergics.
• Anticholinergic Drugs: decreases the activity of
acetylcholine
 benztropine mesylate (Cogentin)
 trihexyohenidyl HCl (Artane)
Other drugs to manage PD:
• Antihistamine – decreases rigidity
 Benadryl
• Betablockers – decreases rigidity
 Inderal