Term
| at what % occupancy of the dopamine D2 receptor does the EPS become a problem? |
|
Definition
|
|
Term
| what is the first 2nd generation antipsychotic? |
|
Definition
|
|
Term
what is the differeince in antagonism profile of clozapine compared to 1st generations-2?
what does this mean? |
|
Definition
less D2
more 5HT 2A
can help postivie and negative symtpoms |
|
|
Term
| which drug is good for severely ill, treatment resistant pts? |
|
Definition
|
|
Term
| what are some additonal effects of clozapine?-4 |
|
Definition
cnitivognition
anti-suicidal
less EPS
less hyperprolactin |
|
|
Term
|
Definition
|
|
Term
| what is clozapine an antagonist for? |
|
Definition
|
|
Term
| major drawbacks for clozapine-4 |
|
Definition
heamtoxicity (agranucytosis)
seizures
myocarditis
metab syndrome |
|
|
Term
| why might the blockage of 5HT 2A be helpful for schiz? |
|
Definition
| can release the normal DA brake and increase DA communicaiton |
|
|
Term
| how does 5HT2A block reduce positive symtpoms? |
|
Definition
| because it reduces glutamatergic activity with lowers DA activity |
|
|
Term
| how does the 5HT2A block reduce negative symptoms? |
|
Definition
| the block of the 5HT2A recpt in prefrontal cortex reduces DA brake |
|
|
Term
| how does 5HT2A blocking reduce the EPS? |
|
Definition
| by relieving DA in striatum to promotoe a little DA signaling to prevent >80% occupancy |
|
|
Term
recpetor occupany with 5HT and DA blockers for:
D2 recptotr
5HT 2A receptor? |
|
Definition
less D2 (around 60% not ever 80)
about 90% |
|
|
Term
how does the 5HT anatgonism affect prolactin?
what is the effect of it with the D2 blocker? |
|
Definition
it decrease prolactin
makes for a more improved release of prolactin as D2 blocker susually increases |
|
|
Term
most aytpical antipsychotics have what type of occupation time fast or slow off?
which ones have medium? |
|
Definition
a fast off
olanzipine
sertindole |
|
|
Term
| what is the side effect that is rare in olanzapine but common in clozapine? |
|
Definition
|
|
Term
| what is the generic of Zyprexa |
|
Definition
|
|
Term
what is teh recptor potency for olanzapine
:
D2
5HT
M1
H1
A1 |
|
Definition
5x better D2
= 5HT
more M1 and H1
less a1 |
|
|
Term
| what are the main ADEs of olanzapine? -3 |
|
Definition
increased appetite/wt gain
drowsiness
dry mouth |
|
|
Term
|
Definition
|
|
Term
what is the affinty of recpetors for risperidone:
5HT2A
D2
M1
H1
a1 |
|
Definition
high
10x better than olanzapine
no affinty
++
+++ |
|
|
Term
| what drug is metabolized by 2D6 |
|
Definition
|
|
Term
| other 5HT2A recpetor drugs: |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| what are the aytpical antipsychotics |
|
Definition
olanzipine
clonzapine
risperidone
ziprasidone
quetapine |
|
|
Term
| common charactersitcs of the atypicals besides clonzapine:-2 |
|
Definition
high affinity of 5HT2A recpt: little parkinsons/prolactin
antiemetic
cogntiive improves |
|
|
Term
| main ADEs of atypicals besides clonzapine-4 |
|
Definition
| sedation, wt gain, mtab syndrome, QT prolong |
|
|
Term
|
Definition
|
|
Term
receptor affinity for aripiprazole:
D2
5HT 2A
5HT 1A
M1
a1
H1 |
|
Definition
partial agonist of D2
full anatg at 5HT2A
partial agonist at 1A
low affintiy for all else |
|
|
Term
| what is the hlaf life like for abilify |
|
Definition
|
|
Term
| what are teh side effects like for abilify |
|
Definition
|
|
Term
which drug is an agonist for 5HT 1A
what does this do |
|
Definition
|
|
Term
| which med is a aprtial D2 agonist/antagonst |
|
Definition
|
|
Term
where are the antipsychotic effect of classical antipsychots seen at for D2 blockade?
what parts of the brain have normal amts of DA-2 |
|
Definition
mesolimbic
pituitary, striatum |
|
|
Term
| which aytpicals have a short half life of 5 hrs? |
|
Definition
|
|
Term
| what are the PK elements of the atypical antipsy-3 |
|
Definition
lipophillic
long half life
high VD and prot binding |
|
|
Term
| what is the sublingual antispychotic? |
|
Definition
|
|
Term
|
Definition
|
|
