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23 Cards in this Set

  • Front
  • Back
Levodopa
Type?
Application?
Contras?
Adverse?
Dopamine precursor
Parkinsons
Effects: dyskinesia, heart diseas, orthostatic HTN
Cx: melanoma, glaucoma, MAO-Is
Levodopa
therapeutic
type?
needs carbidopa
tolerance
Dopamine pre-cursor
Bromocroptine
Pergoglide
Type?
Application?
Contras?
Adverse?
Dopamine Receptor Agonist
parkinsons, galactorrhea
seizures
Cx uncontrolled HTN
bromocriptine
pergoglide
therapuetic?
Receptors targeted?
ergot alkaloid
Bromo: D2 agonist
Pergolide: D1, D2
dopamine agonist
Act primarily on
Pramipexole
Ropinirole
Type?
Application?
Contras?
Adverse?
Dopamine Receptor Agonist
parkinsons
dyskineisa, orthostatic htn
Cx: other sedatives
Pramiprol
Ropinirole
therapeutics?
Receptor Targets?
dopa agonists thathave half lives longer than that of levo
non-ergot
Pramiprol: D3
Ropinirole: D3
Rasagiline
Selegiline
Type?
Application?
Contras?
Adverse?
Inhibit Dopamine Metabolism
Parkinsons
AE: BBB, GI hemorrhage
Cx: cyclobenzaprine
dextromethorphan
meperidine
Rasagiline
Selegiline
Therapeutics?
Type?
MAO blockers
selegiline: MAOB selective at low doses..
toxic metabolite amphetamine
rasagiline: MAOB no metabolite
Tolcapone, Entacapone
type?
Application?
Contras?
Adverse?
COMT blockers.. prevent degradation of DOPA to DOPAC to HVA
parkinsons
dyskinesia
hallucinations
Cx: rhabdomyelosis
liver disease
Entacapone
Tolcapone
therapeutics
tolca: BBB crosser, COMT inhib
entaca: non-BBB COMT inhib
Amantadine
type?
Application?
Contras?
Adverse?
Inhibits NMDA receptors
parkinsons, influenza A
neuroleptic malignant syndrome
Cx: hypersens
Amantadine
therapeutics?
Type?
treats levodopa dyskinesia
inhibits NMDA receptors
trihexyphenindyl, benzotropine
type?
Application?
Contras?
Adverse?
Muscarinic receptor antagonists
parkinsons
SEs: intraocular pressure
Cx: narrow angle
Major metabolite excreted in urine of Dopa degradation?
2 pathways..
2 breakdown enzymes..
Homovanillistic acid (HVA)
1. COMT
DOPA > 3MD > HVA
2. MAO
DOPA > DOPAC > HVA
D1 dopamine receptor
Distribution?
Activity?
striatum, neocortex
excitatory
D2 dopamine receptor
Distribution?
Activity?
Striatum, SN, anterior pituitary gland
inhibitory
D3 dopamine receptor
Distribution?
Activity?
Nucleus Accumbens (reward center), Hypothalamus
inhibitory
D4 dopamine receptor
Distribution?
Activity?
Frontal Cortex, Medulla Midbrain
inhibitory
D5 dopamine receptor
Distribution?
Activity?
Hippocampus, Hypothalamus
excitatory
excitatory D1 type dopamine receptors do..?
inhibtory D2 type dopamine receptors do...?
E: increase cAMP, PIP2 (in Ca++, increase PKC)
I: dec cAMP, Increas K+, decrease Ca++
transporter that moves L-Dopa into brain?
long-chain neutral amino acid transporter (saturable)
Rate limiting step in dopamine synthesis?
Enzyme that turns L-DOPA to Dopamine? (+co-factors)
Tyorsine to L-DOPA (tyrosine hydroxylase)
AADC (aromatic L-amino acid decarboxylase) target for carbidopa
Dopamine to NORE..
enzyme and cofactors? location.
Dopamine Beta-hydroxylase
vitaminc C