Pharm: Parkinson's Disease

Front 1

What is the mechanism of action of Selegiline?

Back 1

It inhibits MAO-B...thus preventing the conversion of Dopamine to DOPAC (and also 3-methoxytyramine's conversion to Homovanillic acid).

Front 2

This drug is metabolized to amphetamine and metamphetamine?

Back 2

Selegiline

Front 3

This drug may be used as 1st Treatment to slow the progression of Parkinson's disease.

Back 3

Selegiline

Front 4

What are the types of administration for Selegiline?

Back 4

PO (per oral) or sublingual

Front 5

In order for selegiline to affect MAO-B only, you should use a (low or high) dose?

Back 5

Low dose is selective for MAO-B

Front 6

Adverse effects of Selegiline include?

Back 6

Sleep disturbances, vivid dreams, nightmares.

Front 7

L-Dopa can be given with to other drugs. What are they? What is their mechanism of action?

Back 7

Carbidopa and Benserazide. They are peripheral L-dopa decarboxylase inhibitors. (So L-dopa doesn't get converted to Dopamine peripherally, allowing L-dopa more opprotunity to get converted to Dopamine in the CNS where it's needed).

Front 8

Vitamin B6 is also known as?

Back 8

Pyridoxal Phosphate

Front 9

What does Pyridoxal Phosphate do?

Back 9

It is a coenzyme for L-Dopa Decarboxylase.

Front 10

If someone is about to take an L-Dopa/Carbidopa treatment, what must you tell the patient to avoid taking?

Back 10

Pyridoxal Phosphate (Vitamin B6).
Why? It will attempt to enhance the function of L-Dopa decarboxylase (which goes against Carbidopa's attempt of inhibiting it peripherally, thus negating the treatment).

Front 11

If you don't use combination therapy in treating Parkinson's disease, one possible adverse effect would be?

Back 11

On-off condition.

Front 12

How do you avoid the adverse effects of On-off condition, for example, that result from taking L-Dopa/carbidopa treatment.

Back 12

Give a combination therapy (continuous Dopamine receptor stimulation is the goal).

Front 13

Your patient comes to you and says "Hey, this previous prescription you gave me, the 'L-Dopa/Carbidopa' treatment. But now I want more central L-Dopa available to get converted to Dopamine, what can you give me?"

Back 13

You'd use a COMT inhibitor.

Entacapone acts peripherally (this blocks conversion of L-Dopa to 3-O-methyldopa, thus leaving more L-Dopa around to eventually reach CNS).

Note: Tolcapone (another COMT inhibitor) acts both centrally and peripherally. I think this should also be able to work in this patient's case.

Front 14

What does it mean when a drug is described as neuroprotective?

Back 14

It slows the progression of the disease for a time

(the term was used in Parkinson's Disease lecture/notes)

Front 15

The F(oral) of L-Dopa is (high/low?)

Back 15

L-Dopa has a low oral bioavailability.

Front 16

This drug is used to inhibit COMT centrally and peripherally.

Back 16

Tolcapone

Front 17

This drug inhibits COMT peripherally.

Back 17

Entacapone

Front 18

What is an adverse effect of Tolcapone?

Back 18

Hepatotoxicity

Front 19

Liver failure might result from which drug (that can be used in the treatment of Parkinson's disease)?

Back 19

Tolcapone

Front 20

What is the mechanism of action of Amantadine WITH RESPECT to treatment for Parkinson's Disease?

Back 20

It's not definitive.
Alter dopamine release and may block reuptake.

But as an antiviral, it blocks M2 H+ channel.

NMDA antagonist

Front 21

This drug is an NMDA antagonist.

Back 21

Amantadine

Front 22

Adverse effects of Amantadine include (5 things).

Back 22

Livedo reticularis (medium sized veins in lower extremities swell, and you get a purplish lace like appearance there).

Ankle edema
Confusion, hallucinations, sleep disturbances.

Front 23

Dopamine agonists can be used with Dopamine precursurs to help limit/prevent what?

Back 23

On-off condition

Front 24

Name the Dopamine agonists that are ergot derivatives.

Back 24

Bromocriptine and Cabergoline

Front 25

Name the Dopamine agonists that are non ergot derivatives.

Back 25

Ropinrole and Pramipexole

Front 26

Last effort to counteract Adverse effects of L-Dopa is?

Back 26

Deep brain stimulation of the subthalamic nucleus.

Front 27

Aside from Parkinson's disease, what else can you use Bromocriptine for?

Back 27

Acromegaly and Fertility control.

Front 28

Bromocriptine can (increase/decrease) fertility, and (increase/decrease) prolactin release.

Back 28

Increase fertility
Decrease prolactin release

Front 29

Which dopamine agonist has a 65 hour half life?

Back 29

Cabergoline

Front 30

Of the Dopamine agonists, which is most likely to increase the incidence of dyskinesias, and why?

Back 30

Cabergoline, because of the the dopamine agonists, it has a higher affinity for D1 receptors (which when activated, can be associated with dyskinesias).

Front 31

CYP1A2 metabolized which dopamine agonists?

Back 31

Bromocriptine, cabergoline, and ropinrole.

Front 32

These dopamine agonists have a lower incidence of dyskinesias.

Back 32

Bromocriptine, Ropinrole, Pramipexole.

Front 33

Pulmonary fibrosis is associated with (ergot/non ergot) derived DA agonists.

Back 33

Ergot derived dopamine agonists.

Front 34

The Mechanism of Action of the Dopamine Agonists affects which receptor primarily?

Back 34

Predominently D2

Front 35

Where do Dopamine agonists act (with regard to MOA)?

Back 35

Limbic system, striatum, and cortex (so the effects are widespread).

Front 36

Bromocriptine stimulates the release of what in normals?

Back 36

Growth hormone

Front 37

Bromocriptine suppresses the release of what in acromegalics?

Back 37

Growth hormone

Front 38

Adverse effects from long term use of ergot derivatives include (3)

Back 38

Valvular Heart Disease
Pulmonary Fibrosis
Retroperitoneal Fibrosis

Front 39

A female gets nauseous taking bromocriptine orally, she can choose to use what other form of administration?

Back 39

Intervaginal

Front 40

A female pt wants to get her hands on some bromocriptine, but she has GERD...what other route of administration could she use?

Back 40

Intervaginal

Front 41

True/False: Dopamine agonists need to be metabolized to an active form.

Back 41

False.

Front 42

True/False: Dopamine agonists enter the brain by the same route of L-dopa/carbidopa, thus they compete for uptake into the CNS.

Back 42

False, False (so, false to both halves of the statement)

Front 43

Constipation, xerostomia, dry skin, confusion, memory impairment, and dysphagia are all adverse effects of what group of drugs? Name the specific drugs in that group.

Back 43

Anticholinergic drugs.

With respect to Parkinson's Tx:
Trihexyphenidyl, Orphenadrine, Benztropine

Front 44

Name a drug that can treat severe tremor.

Back 44

Trihexyphenidyl
Orphenadrine
Benztropine

Front 45

This is used to treat acute dystonias caused by anti-psychotic drugs.

Back 45

Benztropine

Front 46

This is used to treat acute dystonias caused by NEUROLEPTIC???

Back 46

Trihexyphenidyl