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47 Cards in this Set

  • Front
  • Back
What effect does dopamine has on the three different systems (i.e. mesocortical, tuberoinfundibular, and nigrostriatal)?
- Mesocortical: executive function, low DA results in schizophrenia.

- tuberoinfundibular: controls release of prolactin.

- nigrostriatal: intergrate sensory with movement, feeling and emotion, initiate movements.
What does the imbalance of ACh and DA cause?
High level of nonspecific motor output and decrease in voluntary motor output.
What are the two reasons why you only see symptoms with Parkinson's when there is over 80% terminal depletion?
1. Receptor supersensitivity: loss of neuron results in better coupling of DA to receptors and increasing in the number of DA receptors, thus mask the deficit.

2. Increase in firing rate of the remaining neurons: negative feedback loop from SNc to SNr to disinhibit inhibition.
What are some classes of drugs that treat Parkinson's? (6)
1. Anticholinergics: Benztropine, Trihexaphenidyl, Diphenhydramine.
2. Direct DA: L-Dopa, Carbidopa.
3. Direct DA receptor agonist: Bromocriptine, Ropinirole, Piramipexole.
4. MAO-B inhibitor: Selegiline, Rosagiline.
5. COMT inhibitor: Tolcapone.
6. Amantadine
When is anticholinergics usually used in treating Parkinson's?
When disorder is associated with schizophrenics, or DA is contraindicated (low angle glaucoma, prostatic hypertrophy).
Which drug when injected, can treat acute DA blocker induced dystonia such as torticholis and ocular gyric crisis?
Diphenhydramine
What is the key consideration of L-Dopa dosage in treating Parkinson's?
Must start out low and must be titrated to the individual patient.
What is the rate limiting enzyme in DA synthesis in the body?
Tyrosine hydroylase
What are some side effects of L-Dopa?
- initial nausea, vomit
- hypotension
- cardiac arrythmia
- sensory disturbance
- affective disturbance: schizophrenia, paranoia
- increased sexual activity
- dystonia: facial tics, grimace, rocking motions
What is the function of Carbidopa?
inhibit peripheral conversion from L-DOPA to DA.
What are some drug interactions with L-DOPA/Carbidopa?
- B6(pyridoxine): increase the activity of AAAD in the periphery.
- antipsychotics: DA blockers
- nonspecific MAO inhibitors: hypertensive crisis.
- mutual enhancement effects between L-DOPA and anticholinergics.
Why should pyridoxine not be used with L-dopa/Carbidopa?
Pyridoxine(B6) increases the conversion from L-DOPA to DA in the periphery, thus limiting the amount of L-DOPA into the CNS.
Why is nonspecific MAO inhibitor not used with L-dopa/Carbidopa?
Will cause hypertensive crisis.
What is Amantadine used for?
- prophylactic for A2 influenza
- addon drug for Parkinsons': weakly block NMDA glutamate receptors.
What are some dopamine receptor agonists? and which specific receptor do they act on?
- Bromocriptine: D2 agonist
- Ropinirole: D3 agoinst
- Pramipexole: D3 ad D4 agonist
Which of the following will cause sedation?
A. Bromocriptine
B. Ropinirole
C. Pramipexole
C. Pramipexole is also an alpha2 agonist which lowers NE release, thus leads to sedation.
Which of the following will cause less dystonia side effects?
A. Bromocriptine
B. Ropinirole
C. Pramipexole
B. Ropinirole has less binding affinity to D2 and very little affinity to D1, thus do not cause dystonia (an effect of D1 and D2 agonist).
MAO-A inhibitor treats ____ whereas MAO-B inhibitor treats ____.
MAO-A inhibitor treats depression whereas MAO-B inhibitor treats Parkinson's.

MAO-A: degrades NE and Serotonine.
MAO-B: degrade DA only.
What are the two MAO-B inhibitors, and what are their differences?
- selegiline (deprenyl): reversible, metabolized to amphetamine which leads to NE and DA release, causing insomnia and jitteriness especially in elderly.
- rosagiline: irreversible, not metabolized to amphetamine.
Which of the following also treats restless leg syndrome?
A. Bromocriptine
B. Ropinirole
C. Pramipexole
B. Less dystonia.
Which class of drug can be used as adjunctive to increase the "on" time without causing dystonia?
Direct DA receptor agonists, especially Ropinirole.
Name one COMT inhibitor.
Tolcapone: must avoid nonspecific MAO inhibitors, will potentiate L-DOPA side effects such as nausea, anorexia, diarrhea, hallucinations(rare).
D2 dopamine receptors are ____ linked to adenylate cyclase whereas D1 dopamine receptors are ____ linked to adenylate cyclase. (positively/negatively)
D2 dopamine receptors are negatively linked to adenylate cyclase whereas D1 dopamine receptors are positively linked to adenylate cyclase.
What can be used when L-DOPA can no longer be subdivided into more frequent daily doses ("on-off" phenomenon)?
- direct agonists
- MAO-B inhibitors or COMT inhibitors
- anticholinergics
What are some potential treatments for Parkinson's underway?
- transplanted fetal tissue into CNS
- Pallidotomy: only reduces L-DOPA induced dyskinesia.
- Deep brain stimulation
- A2A receptor antagonist(caffeine): decrease GABA neuron firing.
- Coenzyme Q-10: improves mitochondrial electron chain processing for energy production, leading to more firing.
Why are coffee drinkers less likely to develop Parkinson's?
Coffee blocks A2A receptors which modulates GABA neuronal firing.
Which antispastic drugs can be used to treat sprains or strains?
Cyclobenzaprine
Metaxolone
What side effects do cyclobenzaprine and metaxolone have?
Anticholinergic side effects: ataxia, dry mouth, pupil dilation, double vision, urinary retention.
Name one GABA-A and GABA-B agonist. What are their mechanisms of action?
GABA-A agonist: Benzodiazapine

GABA-B agonist: Baclofen
- increase K+ conduction at nerve terminals which then leads to decrease in Ca2+ influx after AP, thus there is less neurotransmitter released to cause muscle contraction.
Name two classes od drugs that can be used to treat spinal cord injury and multiple sclerosis.
1. GABA-B agonist: Baclofen
2. Alpha2 agonist: Tizanidine
Which drug can be used to treat ALS?
Baclofen: GABA-B agonist
Which drug can be used to treat muscle spasm related to stroke?
Tizanidine
What side effects does Baclofen has?
Sedation, weakness, lassitude, confusion.

Overdose: withdrawal syndrome of anxiety and hallucinations.
What side effects does Tizanidine has?
Sedation, dry mouth, dizziness.
Which antispastic drug has wide uses including muscle trauma?
Benzodiazapine (GABA-A agonist) when used in higher dose than antianxiety.
Which drug has direct muscle aciton?
A. Cyclobenzaprine
B. Benzodiazapine
C. Baclofen
D. Tizanidine
E. Dantrolene
E: decreases Ca2+ from sarcoplamsmic reticulum.

Side effects: muscle weakness, fatigue, dizziness, hepatotoxicity.
Which drug can be used to treat muscle spasm related to stroke?
Tizanidine
What side effects does Baclofen has?
Sedation, weakness, lassitude, confusion.

Overdose: withdrawal syndrome of anxiety and hallucinations.
What side effects does Tizanidine has?
Sedation, dry mouth, dizziness.
Which antispastic drug has wide uses including muscle trauma?
Benzodiazapine (GABA-A agonist) when used in higher dose than antianxiety.
Which drug has direct muscle aciton?
A. Cyclobenzaprine
B. Benzodiazapine
C. Baclofen
D. Tizanidine
E. Dantrolene
E: decreases Ca2+ from sarcoplamsmic reticulum.

Side effects: muscle weakness, fatigue, dizziness, hepatotoxicity.
Which of the following drug has potential hepatoxicity?
A. Cyclobenzaprine
B. Benzodiazapine
C. Baclofen
D. Tizanidine
E. Dantrolene
E.
Which of the following is an alpha2 agonist at the bouton?
A. Cyclobenzaprine
B. Benzodiazapine
C. Baclofen
D. Tizanidine
E. Dantrolene
D.
Which of the following antispastic drug can also treat mnalignant hyperthermia and neuroplegic malignant syndrome?
A. Cyclobenzaprine
B. Benzodiazapine
C. Baclofen
D. Tizanidine
E. Dantrolene
E.
Which class of drugs can not be used in combinaiton with MAO-B inhibitors?
Merpiridine and antidepressants: wil cause serotonine(hyperactivity) syndrome.
What drugs can cause medication induced Parkinsonism?
1. antipyschotics(DA antagonist)
2. MPTP(opiod containminants): neurotoxin to substantia niagra.
Which drug can be used to treat MPTP induced Parkinsonism?
MAO-B inhobitors: selegiline or rasagiline.