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FIU - Dopamine receptor
Dopamine receptor
27
Pharmacology
Graduate
12/17/2011

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Cards

Term
which Dopamine receptors increase cAMP, which decrease cAMP
Definition
D1 and D3 increase cAMP
D2, D3, and D4 decrease cAMP
Term
4 classes of D2 blockers
Definition
Phenothiazines, butyrphenones, thioxanthenes, benzamides
Term
phenothiazine
Definition
D2 blockers
"azines"
interact w/ many receptors so many SEs
-H1 - sedation/weight gain
-Mblocker - dry mouth, medriasis, bronchial dilation, tachycardia, constipation, urine retention
-D2 blocker - extrapyramidal SEs
-Alpha blocker - hypotension
-torsades
Term
promethiazine
Definition
D2 blockers
use - pruritis, motion sickness, sedative
"coast guard cocktail" - for motion sickness
Term
prochlorperazine
Definition
D2 blocker
use - drug induced nausea and migraine
Term
fluphenazine
Definition
D2 blocker
antipsychotic
used for long term treatment
Term
butyrphenones
Definition
D2 blockers
more D2 specific than phenothiazines and non-trycyclic
Term
Haloperidol
Definition
D2 blocker - butryphenone
very selective for D2
EPS; dystonic reaction, akinesia, rigidity, tremors, akathisia and tarditive dyskinesia
Term
pseudo-parkinsonism? treatments?
Definition
extrapyramidal symptoms from blocking dopamine -> too much ACh
Tx - anticholinergics: benztropine, trihexiphenidyl, diphenhydramine, amantadine (antiviral)
Term
name the atypical antipsychotics and their metabolism
Definition
Clonzapine - 1A2
Olanzapine - 1A2
Risperidone - 2D6/3A4
Aripiprazole - 2D6/3A4
Quetiapine - 3A4
Ziprasidone - 3A4
Amisulpirid - not metabolized
Term
benztropine
Definition
anticholinergic
anti-parkinson agent
SE - dystonia
Term
trihexyiphenidyl
Definition
anticholinergic
anti parkinsonian agent
Term
diphenhydramine
Definition
antihistamine and anticholinergic
anti-parkinsonian agent
Term
amantadine
Definition
antiviral
anti-parkinson agent
Term
clozapine
Definition
atypical antipsychotic
Low D2, high D4 affinity and 5HT2 antagonist
CYP 1A2 metabolism
SE - agranulocytosis, hypersalivation and hyperthermia, seizures, weight gain (10x10), trycyclic effects
Term
Olanzapine
Definition
atypical antipsychotic
low D2, high D4, 5HT2 antagonist
CYP 1A2 metabolism
SEs - (clozapine w/ NO agranulocytosis) hypersalivation, hyperthermia, seizures, weight gain, trycyclic effects
Term
ziprasidone
Definition
atypical antipsychotic
5HT2 antagonist, NaSRI
3A4 metabolism
SE - QT prolongation - torsades
Term
Quetiapine
Definition
atypical antipsychotic
equal D2 blocker and 5HT2 blocker
3A4 metabolism
SEs - sedation, cataract development and hypothyroidism
Term
Aripiprazole
Definition
5HT2 antagonist, 5HT 1A partial agonist, D2 partial agonist,
2D6/3A4 metabolism
Less weight gain
Term
Parkinson therapy mechanisms
Definition
increase DA by giving DA or a DA-R agonist
Term
2 classes of DA receptor agonsits? examples? SEs
Definition
Ergotamine Derivatives - Bromcriptone and Pergolide. SEs - hallucinations, psychosis, confusion, N&V, postural hypotensioin, fibrosis, vasospasm, GI ulceration
Non-ergotamine derivatives
Pramipexole and Ropinrole
SEs - hallucinations, psychosis, confusion, N&V, postural hypotension, GI ulceration, NO fibrosis, NO vasospasm
Term
bromcriptine
Definition
DA receptor agonist, Ergotamine derivative
Parkinson Disease
Term
Pramipexole
Definition
DA receptor agaonist, non-ergotamine derivative
Parkinson Disease
Term
Ropinrole
Definition
DA receptor agonist, non-ergotamine derivative
Parkinson Disease
Term
Enracapone
Definition
COMT inhibitor (prevents inactivation of levodopa in brain)
Parkinson diseease tx
Term
carbidopa
Definition
inhibits DDC, allowing levodopa to go to brain
Term
Stabilizing levodopa (Stalevo)
Definition
carbidopa, levodopa, and entacapone
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