PD Drugs

Question 1

Apomorphine

Answer 1

dopamine agonist

Question 2

Role of Dopamine agonists

Answer 2

important role as first-line therapy for PD
lower incidence of response fluctuations and dyskinesias that occur with long term LD therapy

may also be given to patients who are taking LD and who have end of dose akinesia or on-off phenomenon or becoming resistant to LD

Question 3

Dopamine Agonists

Answer 3

Apomorphine
Bromocriptine
Pergolide
Pramipexole
Ropinirole
Rotigotine

Question 4

why is Pergolide a dopamine agonists no longer available

Answer 4

has been associated with the development of Valvular heart disease

Question 5

Pramipexole

Answer 5

ergot derivative
preferential affinity for the D3 family of receptors

effective as monotherapy for mild PD but also helpful in patients with advanced disease permitting reduction of LD dose and smoothing out response fluctuations

Readily absorbed after oral administration
Peak plasma after 2 hrs
excreted in the urine

start as dose of 0.125 mg 3x/d
doubled after 1 week and again after another week

Further increments in the daily dose are by 0.75mg weekly intervals depending on response

Most patients require between 0.5 to 1.5mg 3x/d

wof: renal insufficiency may need dose adjustment

Question 6

Ropinirole

Answer 6

nonergoline derivative
pure D2 receptor agonist effective as monotherapy in patients with mild disease and as a means of smoothing the response to LD in patients with advanced disease

0.25 mg 3x/d and the total daily dose is then increased by 0.75 mg/week until the 4th week then 1.5mg/week thereafter

usually 2 -8mg 3x/d is necessary
metabolized by CYP1A2

Question 7

Rotigotine

Answer 7

dopamine agonist
delivered thru a skin patch
approved for treatment of early PD
efficacy in more advanced disease is less clear

Question 8

Adverse effects of dopamine agonists

Answer 8

nausea, vomiting, anorexia
postural hypotension
cardiac arrhythmia is an indication for discontinuation
pergolide - cardiac valvulopathy
dyskinesias
mental disturbances - includes compuslive gambling, shopping, betting, sexual activity
somnolence particularly pramipexole, ropinirole

Question 9

Contraindications to Dopamine Agonists

Answer 9

psychotic illness

recent myocardial infarction or with active peptic ulceration

Question 10

Difference of MAO-A and MAO-B inhibitor

Answer 10

MAO A - metabolizes norepinephrine, serotonin and dopamine

MAO B - metabolizes dopamine slectively

Question 11

MAO B inhibitors

Answer 11

Selegiline
may reduce mild on-off or wearing-off phenomenon

Rasagiline more potent than selefgline in preventing MPTP-induced parkinsonism and is being used for early symptomatic treatment

Question 12

Standard dose of selegiline

Answer 12

5mg with breakfast and 5mg with lunch, may cause insomnia when taken later during the day

Question 13

dosing of rasagiline

Answer 13

1mg/d

Question 14

considerations when giving MAO B inhibitors

Answer 14

not to be given in patients on meperidine, should be used with care in patients receiving tricyclic antidepressants or SSRI - serotonin syndrome

combination of LD and MAOIs must be avoided because it may lead to hypertensive crises because of peripheral accumulation of norepinephrine

Question 15

COMT

Answer 15

Catechol-O-Methyltransferase Inhibitors
tolcapone and entacapone
diminish peripheral metabolism of LD

Question 16

Why is Entacapone preferred over tolcapone

Answer 16

it has not been associated with hepatotoxicity

additional info: tolcapone has central and peripheral effects, entacapone - peripheral

Question 17

Stalevo

Answer 17

LD/CB/entacapone
prep 50 :
 50mg LD/12.5 CB/200mg entacapone 
100:
100mg/25 mg/200mg
150:
150/37.5/200

Question 18

Potent dopamine agonist effective for teoprary relief of off-periods of akinesia in patients optimized dopaminergic therapy
subcutaneous injection

Answer 18

Apomorphine

leading to cinical benefit that begins within 10 minutes of injection and persists for up to 2 hrs

max 10mg, not be given more than 3x daily

Question 19

antiviral agent found to have antiparkinsonism properties

Answer 19

amantadine

MOA unclear
reported to antagonize the effects of adenosine at adenosine A2A receptors, which are receptors that may inhibit D2 receptor function

less efficacious than LD
100 mg 2 or 3x daily

Question 20

Adverse effects of Amantadine

Answer 20

restlessness, depression, irritability, insomnia, agitation, excitement, hallucinations, confusion

overdosage ay produce acute toxic psychosis
higher doses - convulsions

Livedo reticularis
peripheral edema
headache
heart failure
posturla hypotension
urinary retention
GI disturbances

Question 21

<p>dopamine agonistsergot derivatives</p>

Answer 21

<p>ropinirOLE
pramipexOLE
dapat rOLE models pag dopa agonists</p>

Question 22

glutamate antagonist

Answer 22

amantadineantagonist si Amantadine

Question 23

<p>anticholinergics</p>

Answer 23

<p>Benztropine

| Trihexyphenidyl</p>

Question 24

COMT inihibitor

Answer 24

EntacaponeCOMTacapone

Question 25

<p>MAO inihibitors</p>

Answer 25

<p>Rasagiline
Selegiline

M(AOI) RSe</p>

Question 26

side effects of this PD drugLeg swelling, congestive heart failure, prostatic outlet obstruction, confusion, hallucinations, insomnia

Answer 26

amantadine

Question 27

side effects

Atropinic effects: dry mouth, urinary outlet obstruction, confusion, and psychosis

Answer 27

Benztropine

Question 28

aside from levodopa what PD drug can also cause dyskinesias

Answer 28

Entacapone

Question 29

<p>decarboxylase inhibitors</p>

Answer 29

<p>carbidopa

| benserazide</p>

Question 30

True or False

Dopamine agonists are less potent than levodopa.

Answer 30

True

1091

Question 31

True or False

In PD, the use of a low-protein diet has been advocated as a means of controlling the motor fluctuations.

Answer 31

True

p1093