Pharm, Antipsychotics, Linger Flashcards
atypical antipsychotics
ariprprazole lurasidone olanzapine quetiapine risperidone ziprasidone
special use atypical antipsychotics
clozapine
typical low potency agents for antipsychotic
chlorpromazine
typical high potency agents for anitpsychotic
haloperidol
chlorpromazine
dopamine R antagonist
most widely used type of antipsychotic
atypical like clozapine
dopamine R densities in schizophrenics
increased
phenothiazine derivative
chlorpromazine
butyrophenone derivative
haloperidol
common pharm attribute of atypical antipsychotics
greater effects at 5HT2a than at D2 R
most are partial agonists at 5HT1a which is synergistic with 5 HT2a R antagonisms
PK antipsychotics
first pass meatbolism
highly lipid soluble and protein bound
longer clinical duration than estimated
discontinuation well tolerated
which antipsychotic does not have a well tolerated discontinuation
clozapine
cause cholinergic rebound, and movement disorders
metabolism antipyschotics
cytochrone P450
all effective antipsychotics block what R
D2
atypical antipsychoitcs block what R more than D2
5-HT2a
mesolimbic-mesocortical pathway
involved in behavior and cognitive function
cell bodies in ventral tegmental area
antipsychotic if inhibit dopaminergic acitivy in pathway
nigrostriatal pathway
coordination voluntary movement
striatum
inhbition of dopaminergic activity causes extrapyramidal side effects
tuberoinfundibular system
regulates prolactin release (dopamine is inhibitory)
arcuate and periventricular nucli project hypothal and post pituitary
adverse effect if anti dopamine works in tuberinfundibular system
hyperprolactinemia
d2 like dopamine R
D2-4
how do d2 like R work
decrease cAMP via Gi and inhibit Ca Ch, open K Ch
pre and post synaptically and in caudate putamen
typical antipsychotics need what occupancy of D2 R to be effective
60%
extrapyramidal side effects from D2 antagonists occur at waht saturation
> 80%
how can aripiprazole inhibit D2 with no EPS
partial agonist at D2
what reduces suicide attempts in schizophrenics
clozapine
nonpsych indications for antipsychotics
antiemesis
neurleptanesthesia
sleep onset and maintanence
first line for schizoprenia
atypical antipsychotics (not clozapine or olanzapine)
what is used for maintenance of uncooperative patients
IM formualations
haloperidol decanoate, fluphenazine decanoate, Risperdal consta
side effect clozapine
agranulocytosis
dose related lowering of seizure threshold
myocarditis
disadvantage to risperidone
EPS at high dose
hypotension at high dose
disadvantage olanzapine
weight gain
dose related lowering seizure threshold
disadvantage questiapine
high dose if assoc hypotension
twice day dosing from low halt life
advantage questiapine
less weight gain
disadvantage ziprasidone
QT prolongation
which antipsychotics have lower weight gain
quistiapine
ziprasidone
aripiprazole
Tx for how long before full effect
16-20 weeks
electroconvulsive therapy
in adjunct for treating mood Sx and + Sx
can augment clozapine if max dose ineffective
behavioral effects of antipsychotics
older drugs: anhedonia cannot expierieve pleasure, akinesia, toxic confusional state, sedation of antimuscarinic drugs
early motor effects from antipsychotics
EPS like parkinsonism, increased acitivity (akathisia), acute dystonic reactions, dystonic reactions
what is used to Tz early dystonic features of antispychotics
anticholinergic like benztropine or antihistamine antimuscarinic.
NEVER levodopa
late motor effects antipsychotics
tardive dyskinesia, choreathetoid movements
imabalance
which drugs have lower risk tardive dyskinesia
questiapine or clozapine
if drug change or reduction does not help with tardive dyskinesia next step is to
remove all drugs with central anticholinergic acivity like tricyclic antidepressants,
which antipyschotic may cause seziures
clozapine
ANS effects antipsychoics
older drugs that bind alpha 1 and histamine
leads to anti PAN side effects: dry mouth, loss accomodation, difficulty urinating, constipation and anti alpha adrenergic side effects like orthostatic hypotensions, dizziness, sedation, impotence and failure to ejeculate
weight gain is seen with what antipsychotics
majority
greatest effect with clozapine and olanzapine
be careful in DM because of hyperglycemia and ketoacidosis
intermediate risk weigh gain
iloperidone
paliperidone
quetiapine
risperidone
lowest risk weight gain
aripiprazole
lurasidone
ziprasidone
hyperprolactinemia can cause
amenoorhea galactorrhea
infertility
osteoporosis in women
men: infertility, loss libido, impotence, breast enlargement
which drugs can cause hyperPRL
risperidone and paliperidone
minimal effects on PRL
quetiapine
olanzapine and aripiprazole
is agranulocytosis from clozapine reversible
yes upon discontinuance
what CV medications should be avoided in patients on antipsychotics
antiarrhythmics, and erythromycin because also prolong QT
which antipsychotics preferred in pregnancy
atypical
category C
Neuroepileptic Malignant Syndrome
patients sensitive to EPS
rare but life threatening
acute severe parkinsonism, muscl rigidity, ANS instability and HTN, hyperthermia and keukocytosis
Tx neuroleptic Malignant Syndrome
mm relaxants like diazepam or dantrolene
dopamine agonists like bromocriptine
what antipsychotic overdose is fatal
thioridazine- arrhythmia
