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3.29 Antipsychotics
By Dr. Winsauer
54
Pharmacology
Professional
04/15/2012

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Cards

Term
What is thought to be the underlying abnormality of psychoses?
Definition
excess dopamine activity in the central nervous system
Term
What is the evidence for the hypothesis that dopamine causes psychosis?
Definition
drugs that block dopamine receptors are therapeutic in alleviating psychotic symptoms and sympathomimetics drugs which release dopamine (amphetamine) can induce psychosis
Term
How are most antipsychotics administered?
Definition
orally (IM for certain drugs)
Term
What percent of antipsychotics are bound to plasma proteins?
Definition
95-98%
Term
T/F antipsychotics are in general subject to an extensive "first pass" heapatic metabolism
Definition
true
Term
What are the half-lives of antipsychotics like?
Definition
generally long halfe lives (chlorpromazine t1/2=30 hours)
Term
What percent of psychotic patients respond to typical antipsychotics?
Definition
70%
Term
Aministration of antipsychotics leads to characteristic physical and psychological effects known as _______.
Definition
neuroleptic syndrome
Term
What are the symptoms of neuroleptic syndrome?
Definition
sedation, emotional quieting, psychomotor slowing, affective indifference
Term
What are the MOA of phenothiazines?
Definition
predominately dopamine type 2 antagonists
Term
What are the three types of phenothiazines?
Definition
aliphatics, piperidines, piperazines
Term
What is the MOA of the aliphatics?
Definition
low affinity D2 antagonists that pose an increased risk for autonomic side effects
Term
Name some drugs that are aliphatics.
Definition
chlorpromazine, promazine, triflouropromazine
Term
Name the least effective aliphatic?
Definition
promazine
Term
What is the MOA of piperdines?
Definition
when compared to aliphatics these drugs have a higher affinity for the D2 receptor; however these drugs now have a black box warning on the labeling because they can produce a quinidine-like effect on the heart
Term
Name the piperdines?
Definition
mesoridazine and thioridazine
Term
What is the MOA of piperazines?
Definition
high affinity D2 antagonists that pose an increased risk for extrapyramidal side effects; least sedating of the D2 antagonists
Term
What class of drugs are the least sedating of the D2 antagonists?
Definition
piperazines
Term
Name the piperazines.
Definition
fluphenazine, perphenazine, triflouperazine
Term
What is another name for haloperidol?
Definition
butyrophenone
Term
What is the MOA of haloperidol?
Definition
high to intermediate affinity for the D2 receptor and tehrefore poses increased risk of extrapyramidal side effects; decanoate formulation available
Term
Name the thioxanthines?
Definition
chlorprothixene and thithixene
Term
What is the MOA of the thioxanthenes?
Definition
potent D2 antagonists
Term
Name the three broad clases of typical antipsychotics.
Definition
phenothiazines, butyrophenone, thioxanthenes
Term
What's different about the second generation antipsychotics?
Definition
only weakly antidopaminergic so this reduces the potential for tardive dyskinesia and drug-induced parkinsonism
Term
What are dibenzodiazepines?
Definition
second generation antizychotics that are heterocyclic compounds with extrordinarily mixed receptor binding profiles
Term
Name some dibenzodiazepines.
Definition
clozapine, loxapine, olanzapine
Term
What is clozapine especially useful for?
Definition
helps with negative antipsychotic symptoms
Term
What are the side effects of clozapine?
Definition
agranulocytosis, cardiovascular complications such as myocarditis and cardiomyopathy from chronic treatment
Term
If a patient is experiencing agranulocytosis with clozapine, you can switch them to another dibenzodiazepine without that effect, namely ______.
Definition
olanzapine
Term
What are the sieffects of olanzipine?
Definition
case reports have described incidents of sleepwalking
Term
What is the MOA of benzisoxazole?
Definition
relatively selective 5-HT2A receptor antagonists, but at higher doses have ahloperidol like effects
Term
Name the benzisoxazoles.
Definition
risperidone, paliperidone, ziprasidone
Term
What is teh primary active metabolite of risperidone?
Definition
paliperidone
Term
Name the heterocyclic antipsychotics that do not fit into a category.
Definition
molindone, pimozide, quetiapine
Term
What is the MOA of aripiprazole?
Definition
partial dopamine receptor agonist
Term
Why might a partial dopamine agonist be a better treatment than a dopamine antagonist?
Definition
you reduce the incidence of neurolepsis, parkinsonism-like effects and tardive dyskinesias
Term
What other receptors are affected by antipsychotics besides dopamine receptors?
Definition
many antipsychotics can block peripheral muscarinic receptors, alpha0-adrenergic receptors, and histmaine-1 rectpros
Term
T/F Many antipsychotics can result in weight gain
Definition
true
Term
Which antipsychotic is often used as an antiemetic? How does it work as an antiemetic?
Definition
promethazine (because of its antihistaminic effects)
Term
T/F DA plays a substantial role in the chemoreceptor trigger zone.
Definition
true
Term
What are akathisias?
Definition
unpleasant, subjective responses often characterized as "nervous energy"
Term
T/F Akathisias strongly contribute to noncompliance of antipsychotics.
Definition
true
Term
What is akinesias?
Definition
distinct absence of movement
Term
T/F Tardive dyskinesiasa can occur after taking only a few doses of antipsychotics.
Definition
false; symptoms develop after extended periods of time on antipsychotic drug therapy
Term
What percent of patients taking antipsychotic drug therapy get neuroleptic malignant syndrome?
Definition
1%
Term
What percent of patients who get neuroleptic malignant syndrome end up dying from it?
Definition
20-30%
Term
T/F Neuroleptic malignant syndrome can occur at therapeutic doses.
Definition
true
Term
How long after starting to take antipsychotic meds can you develop neuroleptic malignant syndrome?
Definition
within hours of starting treatment to months of treatment
Term
What are the symptoms of neuroleptic malignant syndrome?
Definition
muscular rigidity, impaired breathing or ventilation, autonomic hyperactivity, extremely high temperatures
Term
What kinds of endocrine abnormalities can be caused by antipsychotics?
Definition
increased serum prolactin, which can lead to amenorrhea, dysmenorrhea, and gynecomastia
Term
What are the cardiovascular effects of taking antipsychotics?
Definition
orthostatic hypotension
Term
What are the two most common drug interactions with antipsychotics?
Definition
the potentiation of CNS depressants such as alcohol, an interaction with OTC meds such as antihistamines
Term
What are contraindications for "typical antipsychotic therapy"?
Definition
blood dyscrasias, parkinsonism, chronic alcoholism, liver disease
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