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
CIs: Amatadine
use with caution in pts with hx of seizures and heart failure
Anticholinergics used for PD tx
- benztropine
- biperiden
- orphenadrine
- procyclidine
- trihexphenidyl
Tx: anticholinergics for PD
may improve tremor and rigidity, little effect on bradykinesia
beta-blockers used for tremor
metoprolol and propranolol (beta 1)
AEDs to tx tremor
pirimidone and topirimate
Pyschoactive drug used to tx tremor
benzodiazepines
IM injection used to tx tremor
botox
drugs used to manage choria in HD pts
- reserpine
- tetrabenazine
- olanzapine
- perphenazine
- haloperidol
neuroletic antipsychotics used for tics
- tetrabenzaine
- haloperidol
- pimozide
alpha-andrenergic tx for tics
- clonidine
- guanfacine
only FDA approved tx for RLS
- prampexole
- ropinirole
MOA: Riluzole
- inhibits glutamate release
- blocks postsynaptic NMDA and kainite-type glutamate receptors
- inhibits VGNaCs
Tx: riluzole
ALS
Tx: penicillamine
wilson’s dz
MOA: Penicillamine
Cu chelating agent
AEs: Penicillamine
- nausea
- vomiting
- nephritic syndrome
- myasthenia
- optic neuropathy
- various blood disorders
tx: potassium disulfide
wilsons dz
MOA: potassium disulfide
reduces intestinal absorption of copper
MOA: Bromocriptine
D2 agonist (ergot alkaloid)