Flashcards in antipsychotics Deck (57):
describe the biological basis for antipsychotic treatments?
involves the hyperactivation of the dopamine system
typical antipsychotics block which receptors?
d2 receptors (AC-inhibited)ari
the typical antipsychotics are largely effective for which type of symptoms?
which type of antipsychotics causes elevated prolactin levels and also produces extrapyramidal symptoms?
________antipsychotics are equally effective but differ in potency/side effects
atypical antipsychotics block D2 receptors and what other receptors which may reduce the EPS and improve efficacy for negative symptoms?
which phenothiazine (low potency typical antipsychotic) has an aliphatic side chain?
What is important to remember about the typical antipsychotics that have a piperazine group in the side chain?
they are POTENT-fluphenazine
low potency typical anti-psychotics have a ______ risk of EPS , but an increased risk of antimuscarinic AEs
name the antipsychotic that has high potency and is a butyrophenone
which antipsychotic is only considered atypical at low doses, but is typical at high doses?
risperidone (5-HT2/D2 antagonist
limited EPS at low doses
name the only approved antipsycotic agent used in children and teens?
name the atypical antipsychotics? (6)
"Atypicals can Occasionally quiet risky zebras"
which atypical antipsychotic is a D2 partial agonist that reduces actions of the full agonist?
which atypical antipsychotic has 5-HT2A antagonist and 5-HT1A partial agonist activity and has lower incidence of side effects?
name the atypical antipsychotic: 5-HT2A, H-HT1A, 5-HT2C/D2 antagonist with limited extrapyramidal symptoms
name the 4 atypical antipsychotics (2nd gen.) with the highest potential for CYP interactions via CYP3A4/2D6
"1, 4, 5, 6"
which 2 atypical antipsychotics have a high risk of causing diabetes and causing weight gain?
"Cheetos & Oreos"
among the atypical antipsychotic drugs, which has the highest risk for EPS?
which two atypical antipsychotics have highest for elevated prolactin level?
among the atypical antipsychotics, which has the highest risk for QT prolongation?
what exactly are extra-pyramidal symptoms?
dystonias (sustained contraction of muscles leading to twisted, distorted postures)
akathisia (motor restlessness)
what is neuroleptic syndrome?
suppression of spontaneous movements & complex behaviors
reduced initiative & interest in environment
decreased manifestations of emotions
psychotic symptoms disappear over time
which antipsychotics can lower seizure thresholds via CNS effects?
low potency phenothiazines (chlorpromazine)
why should you avoid antipsychotics in pts with established breast carcinoma?
antipsychotics ( risperidone) can cause increased prolactin secretion
what part of the brain is thought to be the site of antipsychotic effects?
what class of drugs can decrease the extra-pyramidal side-effects without impacting the therapeutic effects on psychosis?
what are some of the clinical consequences of sustained hyperprolactinemia?
what effects do antipsychotics have on the brainstem?
decreased vasomotor reflexes at low doses
what effects do antipsychotics have on CTZ ?
protects against N/V elicited by activation of dopamine receptors
which typical antipsychotic impairs glucose tolerance and decreases insulin release?
how would you treat the AE of acute dystonia in a pt who was taking antipsychotic meds?
treat symptoms (facial grimacing, stiff neck, oculogyric crisis) with anticholinergic antiparkinsonian agents
how do you treat the AE of akathesia (ants in the pants) from antipsychotic therapy?
decrease the dose of antipsychotic agent
add antiparkinsonian agent
antianxiety agent or propanolol
how do you treat the AE of parkinsonian syndrome with antipsychotic therapy?
treat with anticholinergic antiparkinsonian agents or amantadine
what is neuroleptic malignant syndrome?
extrapyramidal side effect w/ fever, severe parkinsonism w/ catatonia, fluctuations in coarse tremor intensity, autonomic instability
elevated creatine kinase
high mortality (10%)
how do you treat neuroleptic malignant syndrome?
immediate cessation of antipsychotic
dantroline or bromocriptine may help
how do you treat the perioral tremor (rabbit syndrome) caused by antipsychotic meds?
treat with anticholinergics
what is tardive dyskinesia and how long does it take to develop?
stereotyped, repetitive, choreiform movements of face, eyelids, mouth, tongue
This takes months or yrs to develop
how long does perioral tremor take to develop?
months or yrs
how do you treat tardive dyskinesia?
jaundice can happen during the 2nd-4th week with what antipsychotic?
blood dyscrasias (leukocytosis, leukopenia, eosinophilia) are especially important when using which antipsychotic?
"watch clozapine closely"
like weekly CBCs
Leukopenia with clozapine may be a forewarning of impending what?
The bioavailability of antipsychotics increases 4-10xs when given via what route?
what are the exceptions to the rule that most antipsychotics have inactive metabolites?
Several N-methylated metabolites of phenothiazines
describe the PKs of antipsychotics?
highly protein bound
accumulates in high blood supply tissues
crosses placental barrier and enters breast milk
are most metabolites of antipsychotics inactive or active?
typical antipsychotics are metabolized with which CYPs?
Many antipsychotics can inhibit CYP2D6, what are the effects of this?
can raise levels of many TCAs & SSRIs
Raise levels of many other antipsychotics
what classes of drugs treat schizophrenia?
what classes of drugs treats bipolar disorder with psychotic features?
mood stabilizers &/or antidepressants
what is the treatment for major depressive disorder with psychotic features?
ECT &/or antidepressant meds &/or antipsychotics
what is the treatment for psychosis due to substance abuse intoxication/withdrawal?
definitive treatment of substance abuse condition
antipsychotics as an adjunct for delirium
describe how the long acting depot antipsychotics have slow release?
have slow release of the active drug produced by combining the base AP with a fatty acid (decanoic acid)
what happens to the alcohol group of the antipsychotic drug when used in long acting depots?
alcohol group is esterified by the acid producing a lipophilic compound with increased solubility in oil-usually sesame
when should you consider using a depot prep. for antipsychotic therapy?
pts with several relapses who don't take oral meds
pts who have clear cut compliance issues
when oral absorption is poor