MOA A/E Drug/Drug Interactions Contraindications
PARKINSON'S
Peripheral decarboxylase
inhibitor - B/c so much LDOPA
converts outside of brain
this allows to get more Has only a certain amount of time that it will
Cardopa dopamine in brain - work - a few years
Benserazide
Dopamine precursor
only works for a few years - responsiveness
may ultimately be lost completely - GI Pyridioxine (Vit. B6) - more
(nausea & vomiting b/c of central stimulation and more dopamine will be
Gets it across the BBB to be in the CTZ), Cardiovascular effects converted peripherally
able to convert to dopamine (arrhythmias, postural hypotension - getting Monoamine oxidase A
- stimulates D2 receptors in converted to epinephrine and inhibitors - can cause a
the Substania Nigra - give on norepinephrine), Dyskinesias (peak does hypertensive crisis - breaks
empty stomach - effective in when it is first "turned on") Behavioral effects down serotonin, Psychotic patients -
Levadopa relieving bradykinesia (depression, anxiety, hallucinations - b/c of norepinephrine, dopamine Acute Angle Glaucoma
Dopaminergic agonists GI (anorexia, nausea, vomiting), painless
digital vasospasm, Dyskinesias (abnormal
stimulates dopamine - D2 movements similar to Levodopa), Mental
Bromocriptine (ergot) agonist disturbances
directly stimulates both D1
Pergolide (ergot) and D2 painless digital vasospasm
synthetic - relatively pure D2
Ropinirole (non-ergot) receptor agonist
synthetic - preferential
affinity for the D3 family of
Pramipexole (non-ergot) receptors
D3 family - transdermal
Rotigotine (newest) application
MAO-B inhibitor
allows to increase dopamine
in brain b/c it is not allowing
MAO-B to break down the
dopamine - enhances and
prolongs the
antiparkinsonism effect of
Levodopa, neuroprotetive Meperidine - may cause
Selegiline effect serotonin syndrome
Rasagiline MORE POTENT
COMT (catechol-o-
methyltransferase) inhibitor prevents 3-OMD from
breaking down dopamine
allowing for more to remain - dyskinesias, nausea, and diarrhea, abdominal
prolongs action of Levodopa pain, orthostatic hypotension, sleep
by diminishing its peripheral disturbances - orange colored urine -
Entacpone metabolism - increased levodopa toxicity
Tolcapone can enter the BBB can be hepatotoxic
Dopamine facilitator short lived, disappearing after a few weeks;
increases dopamine restlessness, depression, irritability,
availability - antiviral agent - insomnia, agitation, excitement,
may potentiate function by hallucinations, and confusion; livedo
influencing synthesis, reticularis (marbeling red rash); peripheral
Amantadine release, or reuptake edema
Central anticholinergics
Antagonist at M receptors in
basal ganglia - reduces
tremor and rigidity; little sedation, mydriasis, urniary retention,
Benztropine effect on bradykinesia constipation, confusion, dry mouth
decreases acetylcholine -
improve the tremor and
regidity of parkinsonism but
have little effect on
Trihexyphenidyl bradykinesia - muscarinic
(Benzhexol) antagonist elderly males - can have urinary issues
Biperidine
Drug-Induced Parkinsonism
Reserpine Depletes dopamine
Tetrabenazine
D2 antagonist - anti-
Haloperidol psychotic medication
Metoclopramide anti - nausea
Street drug - selectively
taken up by cells in the
Substania Nigra - inhibits
mitochondrial complex 1,
1-methyl-4-phenyl-1,2,3,6- inhibiting oxidative
tetrahydropyridine (MPTP) -- phosphorylation - striatal
> N-methyl-4- dopamine depletion and
phynylpyridinium (MPP+) parkinsonism
HUNTINGTON'S
Dopamine Depleter Deplete amine transmitters,
especially dopamine from
nerve endings; reduce
Tetrabenazine chorea severity Hypotension, Sedation, Depression, Diarrhea
Reserpine
Deutetrabenazine
TOURETTEs Block D2 receptors - reduce Parkinsonism, other dyskinesias; sedation;
vocal and motor tic blurred vision; dry mouth; GI disturbances;
frequency, severity of pimozide may cause cardiac rhythm
Pimozide Tourette syndrome disturbances
Haloperidol
Fluphenazine
RESTLESS LEG
Pramipexole (non-ergot) Dopamine agonist
Ropinirole (non-ergot)
Gabapentin GABA analog
WILSON'S DISEASE Copper chelating agents -
need to get rid of excess
Trientine hydrochloride copper
Penicillamine
MULTIPLE SCLEROSIS
Mitoxantrone immunosuppressant
alpha integrin; prevents T-
Natalizumab cells into the brain
Rituximab CD 20 antibody
shifts the population of T
cells from proinflammatory
to Th1 T-cells to regulatory
Th2 T-cells that supress the
Glatiramer inflammatory response
Beta interferons
Corticosteroids ACUTE manifestations
selective sphingosine-1-
phosphate receptor
Fingolimod modulator
Siponimod
anti-neoplastic (Hairy cell
Cladribine leukemia)
ALZHEIMER'S
Central cholinesterase
inhibitors
Centrally acting and
Tacrine increasing acetylcholine can be very hepatotoxic
Donepezil
Rivastigmine
Galantamine
Glutamate Antagonist
Memantine NMDA antagonist
Inhibitors of microtubule
assembly
Epothilone - D
The treatment for Lewey
Body dementia is the same
as Alzheimers
ALS
Na+ channel blocker on the
Riluzole neurons; inhibitor of NMDA
