Exam 11: Antipsychotics Flashcards
4 Phenothiazines
-Azines Chlorpromazine Fluphenazine Prochlorperazine Trifluoperazine
Name 1 Butyrophenone
Haloperidol
6 Second Generation (Atypical) Antipsychotics
Clozapine Olanzapine Risperidone Ariprazole Quetiapine Ziprasidone
What kind of symptoms are 1st generation antipsychotics (Phenothiazines and haloperidol) good at treating?
Positive symptoms of schizophrenia
General effects of typical/1st gen antipsychotics
Decreased initiation of behavior, flattened affect
What is a major problems with the use of antipsychotics that affects their use?
their effects are perceived as unpleasant by the patient
What effect occurs before the antipsychotic effects in treatment?
Sedation
Tolerance develops to the though in time
CNS side effect of antipsychotics
Lowered seizure threshold
Which antipsychotic is also an especially good antiemetic?
Prochlorperazine
Autonomic side effect of antipsychotics
Anticholinergic
2 Cardiovascular side effects of antipsychotics
- Orthostatic hypotension
2. Tachycardia
Endocrine side effects of typical antipsychotics
Increased prolactin due to dopamine antagonism
Gynecomastia, lactation, menstrual problems
May affect other GH, corticosteroids, gonadotropins, insulin
Common unwanted side effect of antipsychotics
Weight gain, metabolic disturbances
How safe are antipsychotics
Very large margin of safety, but there is a small risk of idiosyncratic and allergic reactions that can be serious
Neuro side effects of antipsychotics
Extrapyramidal
Can be severe and limit their use
Mechanism of antipsychotics
Inhibition of DA receptors
Typical inhibit D2
Others may affect other DA receptors/other neurotransmitters
Which DA pathway is involved in psychosis
Mesolimbic and mesocortical systems
Tardive dyskinesia
too much dopamine activity relative to cholinergic activity
opposite of parkinson’s
Aliphatic phenothiazine
Chlorpromazine
3 piperazine phenothiazines
trifluoperazine
fluphenazine
prochlorperazine
Trifluoperazine
Phenothiazine
More potent than chlorpromazine
less sedation/anticholinergic
More extrapyramidal problems
Fluphenazine
Phenothiazine
Comes in long acting injections (decanoate and enathate), good for compliance
Prochlorperazine
Phenothiazine
Commonly used as an antiemetic
Haloperidol
Butyrophenone Less anticholinergic than chlorpromazine more extrapyramidal side effects less sedation Available in long acting form
Clozapine
2nd gen antipsychotic
blocks D4 and 5-HT2 receptors
Can cause granulocytopenia and agranulocytosis*
Can cause weight gain and type 2 diabetes
Strongly anticholinergic
Few extrapyramidal side effects
Very expensive
Olanzapine
2nd gen antipsychotic
like clozapine, but doesnt cause bone marrow toxicity
Also causes weight gain and hyperglycemia
Risperidone
2nd gen antipsychotic
Blocks DA and serotonin receptors
More extra pyramidal side effects than clozapine/olanzapine, but less than the typicals
Quetiapine and Zirprasidone
2nd ben antipsychotics
mechanism similar to clozapine
metabolic side effects (fewer with quetiapine)
Aripiprazole
2nd gen antipsychotic
Partial agonist at D2 and 5-HT1 receptors
No extrapyramidal problems
Also approved for refractory depression
general pharmacokinetics of antipsychotics
metabolized in liver, excreted in kidney
Long half lives
Most effective antipsychotic. Problem?
Clozapine
2nd line due to it’s potential toxicity
General rule of thumb about side effects of antipsychotics
high potency drugs have fewer cardiovascular and anticholinergic effects, but more extrapyramidal effects
the opposite is true of lower potency drugs.
