Drugs for Movement Disorders - Kruse Flashcards
T1/2: Bromocriptine
15 h
Peak [plasma]: bromocriptine
1-3 h
metabolism: bromocriptine
CYP3A4 - extensive first pass
benefit of dopamine antagonist
lower incidence of response fluctuations and dyskinesia in comparison to LT L-dopa tx
MOA: Pramipexole
D3 receptor agonist
Tx; Pramipexole
RLS
peak [plasma]: pramixole
2h
T1/2: pramipexole
8h
ROE: pramipexole
90% in urine
MOA: ropinirole
D2 receptor agonist
tx: ropinirole
RLS
Met: ropinirole
primarily CYP1A2
T1/2: ropinirole
6h
peak [plasma]: ropinirole
1-2h
Dopamine receptor agonists
- bromocriptine
- pramipexole
- ropinirole
AEs: Dopamine Agonists
- GI: anorexia, nausea, vomiting
- postural hypotenstion
- peripheral edema + cardiac arrhythmias = stop using
- more severe mental dist than w/ L-dopa
CIs: Dopamine agonists
- psychosis
- recent MI
- active peptic ulcers
- periperal vascular dz (bromocriptine)
MOA: Selegiline
selective, irreversible MAO-Bi
MOA: Rasagiline
irreversible MAO-Bi, > potent than selegiline
CIs: Selegiline
- merperidine
- tricyclic antidepressants
- SRIs
AEs: Rasagline
hypertensive crisis when used with L-dopa
AEs: Tolcapone
death from acute hepatic failure d/t increase in liver enzymes
MOA: COMTi
competes with L-dopa for transport across membranes - prolongs L-Dopa activity by inhibiting peripheral metabolism
AE: Amatadine
livedo reticularis: purplish mottled disocloration of skin, usually legs