Movement Disorder Drugs Flashcards Preview

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Flashcards in Movement Disorder Drugs Deck (32):
1

Levadopa MOA

Metabolic precursor of DA
Converted to DA by L-aromatic amino acid decarboxylase

2

Contraindications for Levadopa

Pyridoxine (B6)
Do NOT give within 14 days of MAOI
Avoid rapid discontinuation -- causes neuroepileptic malignant syndrome

3

What is the major/common side effect of Levadopa that needs to be considered?

On-Off Phenomenon
Large doses are required due to the peripheral decarboxylation that takes place.

4

Carbidopa MOA

Aromatic L-amino acid decarboxylase inhibitor
Does NOT cross BBB
Dinimishes peripheral L-Dopa metabolism
ONLY used in conjunction with L-Dopa

5

Entacapone MOA

COMT Inhibitor
Reduces metabolism of peripheral levodopa
Does NOT cross BBB
ONLY used in conjunction with L-Dopa

6

Tolcapone MOA

Inhibits peripheral and central COMT
CROSSES BBB
INC CNS uptake of L-Dopa
Used as adjunct in patients on L-Dopa/Carbidopa

7

Contraindications Tolcapone

Side effect: fulminating hepatic necrosis
BLACK BOX warning -- Liver disease lab monitoring

If NO clinical improvement after 3 weeks of therapy (regardless of dose), discontinue tolcapone treatment.

8

Selegiline/Rasalgaline MOA

Selectively inhibits MAO-B
Selegiline -- metabolized to amphetamine (potentiates effects of DA in brain)
Rasalgaline -- MORE POTENT

9

Contraindications for Selegiline/Rasalgaline

Large number of potential drug interactions
Promotes serotonin syndrome so NO use of Serotonin Reuptake Inhibitors
Avoid TYRAMINE -- cheese, draft beer

10

What are the 6 Dopamine Agonists?

Bromocriptine
Pramipexole
Ropinirole
Apomorphine
Pergolide
Rotigotine

11

Bromocriptine

Rarely used Ergot
Combination with L-Dopa

12

Pramipexole

Non-ergot D3 agonist
Mono therapy in MILD PD
Adjunct therapy in advanced PD in combo with levodopa
Restless Leg Syndrome
No appreciable metabolism SO this is a LOWER DOSE for renal insufficiency patients

13

Ropinirole

D2 receptor agonist
Mono therapy in mild PD
Extended release

14

Apomorphine

Rescue therapy or continuous infusions
Nausea common
Treat 3 days before use with antiemetic

15

Pergolide

WITHDRAWN

16

Rotigotine

WITHDRAWN -- crystal formulation at site of patch

17

GI side effects of dopamine agonists

Anorexia
Nausea
Vomiting
Constipation
Dyspepsia
*Most common at BEGINNING of therapy*

18

CV side effects of dopamine agonists

Postural Hypotension
Painless digital vasospasm
*More common at start of therapy, Ergot derivatives*

19

Dyskinesia side effects of dopamine agonists

Similar to levadopa

20

Mental side effects of dopamine agonists

Confusion
Delusions
Hallucinations
Impulse control problems
Compulsive gambling
sex
shopping

21

Other common side effects of dopamine agonists

Headache
Nasal Congestions
Increased arousal
Pulmonary infiltrates
Uncontrollable tendence to fall asleep

*Ergot agonists*

22

Amantadine MOA

Enhances DA synthesis and release
Inhibits DA reuptake
Antiviral drug
Early stages of PD or as a supplement

23

Antimuscarinic Agents

Trihexyphenidyl
Benztropine
Biperiden

*Usually given as primary agents prior to introduction of L-Dopa in younger patients with mild tremor

24

Tetrabenazine MOA

Blocks dopamine reuptake into presynaptic vesicles
Results in dopamine depletion
Reduced dopamine signaling

25

Side effects/Contraindications for Tetrabenazine

Mostly related to dopamine loss -- Parkinsonism
Do NOT use in actively suicidal patients or those with inadequately treated depression

26

Dopamine antagonists (4)

Chlorpromazine
Haloperidol
Risperidone
Olanzapine

27

Baclofen MOA

GABA Analog, GABAb agonist
Muscle relaxant

28

Drug interactions Baclofen

Can enhance CNS depression of other drugs
Contraindications -- Elderly patients

29

Riluzole MOA

Inhibitory effect on glutamate release
Inactivation of voltage-dependent sodium channels
Slows ALS progression to a modest degree

30

What are the drugs of choice for Alzheimer's disease?

AChEI's = DOC
-- can cause insomnia
Tacrine, Donepezil, Galantamine, Rivastigmine

*Interactions = succinylcholine

31

Memantine MOA

NMDA Antagonist
Bings Mg site and thus blocks channel

32

Side Effects/Contraindications for Memantine

Cardia Failure = side effect
Avoid drugs/diets that will change urine pH