Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
27 Cards in this Set
- Front
- Back
|
General MOAs
|
- Replacement therapy
- COMT inhibition - DA releasers - MAO-B inhibition - DA receptor agonists - Anticholinergics |
|
|
Levodopa
|
- Replacement therapy
- only used in combination with carbidopa |
|
|
Carbidopa/Levodopa
|
- Replacement therapy + inhib. of peripheral aromatic L-AA decarboxylase
- carbidopa/levodopa is effective for 2-5 years and then starts to wear off causing "on-off" effect - AE: dose related diskinesia, pathological gambling, peripheral effects (nausea, vomiting), CNS effects (vivid dreams, hallucinations) |
|
|
Tolcapone
|
- COMT inhib.
- Metabolism: glucuronidation - AE: fatal hepatoxicity, diskinesia, nausea, diarrhea, urine discoloration |
|
|
Entacapone
|
- COMT inhib.
- Can lower required dose of carbadopa/levodopa - Metabolism: glucuronidation - AE: diskinesia, nausea, diarrhea, urine discoloration |
|
|
Amantadine
|
- Dopamine releaser, NMDA antagonism
- ClogP = 2.4 - Useful in early stages - Metabolism: unchanged - AE: nausea, dizziness, insomnia, confusion, hallucinations, psychosis at high serum levels (elderly) |
|
|
Selegiline (L-deprenyl)
|
- irreversible inhibition of MAO-B, inhib. dopamine reuptake
- Can lower needed L-DOPA dose - Metabolism: 2B6, 2C19 - N-dealkylation to R-methamphetamine (less potent enant.) - AE: orthostatic hypotension, nausea, insomnia, can exacerbate AEs of L-DOPA - Do NOT use w/ TCAs |
|
|
Rasagiline
|
- MAO-B inhib.
- Metabolism: 1A2 - N-dealkylation to inactive - fewer peripheral AE than selegiline |
|
|
Rasagiline
|
- MAO-B inhib.
- Metabolism: 1A2 - N-dealkylation to inactive - fewer peripheral AE than selegiline |
|
|
DA Receptor Agonists
|
- Less active than L-DOPA
- Less likely to cause dyskinesia or motor fluctuations - Can lower required L-DOPA dose - AE: nausea (blocked by D2 antagonists e.g. domperidone), somnolence, "sleep attacks", toxic psychosis, orthostatic hypotension, confusion, pathological gambling - Sleepiness can be combat w/ modafinil |
|
|
Bromocriptine
|
- DA receptor agonist, 5HT2B agonist, partial D1 full D2 agonist
- Metabolism: 3A4, t1/2 = 3 hrs |
|
|
Bromocriptine
|
- DA receptor agonist, 5HT2B agonist (cardiotoxic), partial D1 full D2 agonist
- Metabolism: 3A4, t1/2 = 3 hrs |
|
|
Pergolide
|
- DA receptor agonist, 5HT2B agonist (cardiotoxicity), Partial D1 full D2 agonist
|
|
|
Ropinirol
|
- DA receptor agonist, full D2 and D3 agonist
- Also for RLS - Metabolism: 1A2 - N-despropyl to inactive |
|
|
Pramipexole
|
- DA receptor agonist, full D2 and D3 agonist
- also used for RLS - Metabolism: 90% unchanged |
|
|
Apomorphine
|
- DA receptor agonist, potent D1 and D2 agonist
- only approved for treatment of hypomobility ("off" episodes) - R-enantiomer - equivalent to L-DOPA in treatment results - Metabolism: extensive 1st pass - AE: similar to L-DOPA, vomiting (give trimethobenzamide 3 days before), hypersexuality |
|
|
Rotigotine
|
- DA receptor agonist, D1 D2 and D3 agonist
- Comes TD patch only - Metabolism: N-dealkylation, sulfonation, glucuronidation - AE: typical for this class |
|
|
Cabergoline
|
- DA receptor agonist
- D2, D3, and potent 5HT2B (cardiotoxic) agonist - Metabolism: minimal CYP involvement, hydrolysis of acyl urea |
|
|
Anticholinergics
|
- Effective in early stages of Parkinsonism
- AE: - Peripheral: tachychardia, can't see, can't pee, can't spit, can't sh*t - CNS: somnelence, hallucinations, impared memory, delusions, ataxia, dysarthria |
|
|
Anticholinergic Drugs
|
- Atropine
- Benztropine - Procyclidine - Diphenhydramine - Trihexyphenidyl |
|
|
Ropinirol
|
- DA receptor agonist, full D2 and D3 agonist
- Also for RLS - Metabolism: 1A2 - N-despropyl to inactive |
|
|
Pramipexole
|
- DA receptor agonist, full D2 and D3 agonist
- also used for RLS - Metabolism: 90% unchanged |
|
|
Apomorphine
|
- DA receptor agonist, potent D1 and D2 agonist
- only approved for treatment of hypomobility ("off" episodes) - R-enantiomer - equivalent to L-DOPA in treatment results - Metabolism: extensive 1st pass - AE: similar to L-DOPA, vomiting (give trimethobenzamide 3 days before), hypersexuality |
|
|
Rotigotine
|
- DA receptor agonist, D1 D2 and D3 agonist
- Comes TD patch only - Metabolism: N-dealkylation, sulfonation, glucuronidation - AE: typical for this class |
|
|
Cabergoline
|
- DA receptor agonist
- D2, D3, and potent 5HT2B (cardiotoxic) agonist - Metabolism: minimal CYP involvement, hydrolysis of acyl urea |
|
|
Anticholinergics
|
- Effective in early stages of Parkinsonism
- AE: - Peripheral: tachychardia, can't see, can't pee, can't spit, can't sh*t - CNS: somnelence, hallucinations, impared memory, delusions, ataxia, dysarthria |
|
|
Anticholinergic Drugs
|
- Atropine
- Benztropine - Procyclidine - Diphenhydramine - Trihexyphenidyl |
