Q2 Antipsychotic Drugs Flashcards
many psychotherapeutic drugs produce their effects by increasing or decreasing the rate of
- neuronal circuit output
antipsychotic drugs in schizophrenia only treat ______ symptoms
which symptoms
- positive
- delusions and hallucinations
antipsychotic drugs are _______ of multiple receptors found throughout the brain and in peripheral tissues
- competitive antagonists
what receptors do antipsychotic drugs antagonize
- D2 dopamine
- 5HT2A serotonin
- M2/3 acetylcholine
- alpha 1 NE
- H1 histamine
- K+ channel in cardiac tissue
the therapeutic effect of antipsychotic drugs is mediated by their _______ of _____ and ______ receptors
- antagonism
- dopamine
- serotonin
some antipsychotic drugs are partial _______ for ____ and _____ receptors
- agonists
- dopamine
- serotonin
first generation antipsychotic drugs are callled
second generation antipsychotic drugs are called
- typical
- atypical
examples of first gen antipsychotic drugs
which are high potency and which are low potency
what does high potency/low potency mean
- fluphenazine (HP)
- haloperidol (HP)
- chlorpromazine (LP)
- high potency - low doses needed
- low potency - high doses needed
examples of second gen antipsychotic drugs
- clozapine
- olanzapine
- risperadone
- aripiprazole
CORA (that creepy cartoon who needed an antipsychotic)
all antipsychotic drugs antagonize or partially agonize the ____ receptor in the _____ pathway which is though to be primarily responsible for their therapeutic inhibition of positive symptoms
- D2 dopamine receptor
- mesocortical
in schizophrenia, hyperstimulation of the ______ pathway which connects the ventral tegmental area to the prefrontal cortex causes excessive ___ to be released into the _____
- mesocorticol dopaminergic
- dopamine
- prefrontal cortex
the correlation between a drug’s affinity for the ____ receptor and its clinical effectiveness is extremely strong
- D2 receptor
drugs with higher D2 receptor affinity require _____ doses to be therapeutically effective
- lower
research has shown that only ____% of the D2 receptors in the prefrontal cortex need to be occupied by a drug in order to produce a maximal clinical response
this is an example of _____ and it indicates that the dose of. drug can be titrated either up or down in order to find an optimal dose for each patient
- 60%
- receptor reserve
while all antipsychotic drugs antagonize the 5HT2A serotonin receptor, the _____ generation drugs do so with higher affinity than the _____ drugs
- this explains
- second generation does so better than first generation
- explains inhibition of positive symptoms by second generation drugs
what toxicity results from antagonism of D2 receptors in non-therapeutic dopamine pathways
- is this more prominent in first or second generation drugs? why?
- extrapyramidal symptoms
- more prominent in first
- second generation has lower affinity for D2 dopamine receptor and antagonize with lower potency than 1st generation drugs
extrapyramidal symptoms involve loss of
examples
- skeletal muscle control
- pseudoparksonism
- acute dystonia
- akathisia
- tardive dyskinesia
inhibition of the _____ pathway is responsible for the extrapyramidal symptoms of antipsychotic drugs
why
- nigrostriatal
- responsible for skeletal muscle movement
antipsychotic drug-induced changes in pituitary hormone secretion particularly _____ may also result from inhibition of dopamine receptors.
is this more common with first or second generation antipsychotic drugs
- prolactin
- more common with first generation antipsychotic drugs
inhibition of the _______ pathway is responsible for the hormonal effects of antipsychotic drugs
how
- tuberoinfundibular pathway
- dopamine released from pituitary gland from tuberoinfundibular neurons to inhibit release of prolactin
effects of hyperprolactinemia
- gynecomastia
- amenorrhea
- decreased libido and sexual function
Also associated with inhibition of dopaminergic (DA) pathways * is ____________ another important potential toxicity of __________ drugs
- neuroleptic malignant syndrome (NMS)
- anti-epileptic drugs
what condition is characterized by muscle rigidity, hyperthermia, and mental status changes such as agitation and dysautonomia
what treats the agitation
what treats the dopamine antagonism
what treats the muscle rigidity and hyperthermia
- neuroleptic malignant syndrome
- Benzodiazepines
- Bromocriptine
- Dantrolene
how does Dantrolene treat muscle rigidity and hyperthermia
- inhibits Ca2+ flow through ryanodine receptor
- reduces skeletal muscle contraction and reduces heat
