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Pharmacology
Dopamine Receptors
16
Medical
Graduate
03/01/2010

Additional Medical Flashcards

 


 

Cards

Term
Types of Dopamine Receptors
Definition

D1 and D5 activate adenylyl cyclase

while

D2, 3, and 4 inhibit adenylyl cyclase

Term
What are dopamine-2 receptor blockers used for?
Definition
neuroleptics/antipsychotics, such as Phenothiazines and Butyrophenones
Term
Phenothiazines
Definition

dirty drug

H1 blocker: sedation

M blocker: dry mouth

D2 blocker: extrapyramidal anti-emetic, prolactin release

alpha blocker: hypotension (orthostatic), nasal congestion

Na and K block: 1a effect = QT prolongation

Term
Butyrophenones
Definition

clean drug

high affinity for D2 receptor, less side effects, but more D2-mediated side effects

but causes Parkinson-like extrapyramidal rigidity, dystonic reaction and hypokinesia --> akinesia --> tremors --> akathisia --> tardive dyskinesia

Term
Pseudo-Parkinsonism
Definition

iatrogenic

 

for treatment, use anti muscarinic - benztropine (atropine-like), trihexphenidyl, diphenhydramine, and amantadine

Term
benztropine
Definition
Term
diphenhydramine
Definition
Term
amantadine
Definition
Term
atypical neuroleptics
Definition

clozapine, risperidone, olanzapine, quetiapine, ziprasidone, sulpirid

 

do not work via dopamine receptors or cause extrapyramidal side effects

Term
Clozapine
Definition

Low(er) affinity for D2
High affinity for D4
High affinity antagonism for 5-HT2

 

metabolism via 1A2

 

but: causes agranulocytosis, sedation, orthostasis, QT prolongation, hypersalivation, hyperthermia, seizures, weight gain, diabetogenic

Term
Olanzapine
Definition

clozapine w/o agranulocytosis and hypersalivation

 

otherwise very similar

Term
Risperidone
Definition

5-HT2 > D2 blocker

 

can induce Parkinsonian side effects at high dose

Term
Ziprasidone
Definition

5HT-2 antagonist

SNRI

QT prolongation

 

no other side effects known

bipolar disorder, schizophrenia

Term
Sulpiride
Definition

D2 blocker, GHB blocker, antidepressive

 

some parkinsonism, dose dependent

amisulpiride = same, w/o weight gain

Term
Quetiapine
Definition

sedating, cataracts, hypothyroidism

 

mixed drug

Term
Aripiprazole (abilify)
Definition
5HT2 antagonist, 5HT1a partial agonist, D2 partial agonist
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