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Pharmacology
Antipsychotic Drugs
31
Medical
Graduate
10/08/2009

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Cards

Term
define antipsychotic
Definition
effectiveness in tx psychosis
Term
define neuroleptic
Definition
production of EPS
Term
what type of drug is chlorpromazine?
Definition
first generation antipsychotic
Term
T 1/2 of chlorpromazine
Definition
30hrs (long)
Term
What receptors does chlorpromazine interact with?
Definition
D2 R antagonist (defining property)
alpha 1 antagonist (hypotension & sexual dysfxn)
M antagonist (autonomic side fx)
H1 antagonist (sedation)
non-competitive channel blocker (calcium, sodium, cardiac side fx)
Term
Behavioral and psychological effects of CPZ: early
Definition
"major tranquiling chemical straightjacket": sedation, disinterest for environment, psychomotor slowing, emotional quieting
Term
Behavioral and psychological effects of CPZ: late
Definition
(2-3wks and 4-6 mths to stabilize): alleviates tension, hyperactivity, hostility, hallcuinations & delusions, anorexia, negativism, and sometimes withdrawal
Term
Neurological side effects: chlorpromazine early onset
Definition
EPS that are reversible and treatable
Parkinson like sx, akathisia, acute dystonic rxns
Term
Neurological side effects: chlorpromazine late onset
Definition
EPS: tardive dyskinesia (irreversible and untreatable!)
Term
Mechanism of action: chlorpromazine
Definition
D2 R antagonist
Term
Anatomical site of antipsychotic effects:
Definition
D2 receptors of frontal cortex and limbic structures
Term
Anatomical site of EPS effects:
Definition
Early on D2 blockade in the striatum -> inc activity of striatal cholinergic neurons
Later on with TD - TD is not alleviate by anti-muscarinic drugs. Don't know the mechanism.
Term
Side effects: chlorpromazine
Definition
Sedation, coma, lowered seizure threshold, alpha1 blockade, quinidine-like effects on heart , neurleptic malignant syndrome
Term
what is neuroleptic malignant syndrome and what is it a side effect of?
Definition
A sydnrome of hyperthermia, diffuse muscle rigidity, autonomic sx, altered consciousness
parenterally administered high potency antipsychotics.
Term
how would you treat neuroleptic syndrome?
Definition
as it results from over-suppression of D2, tx muscle rigidity with muscle relaxant and then with bromocriptine the D2 agonist
Term
Thioridazine is what kind of drug?
Definition
low potency classical antipsychotic
Term
Trifluoperazine is what kind of drug (what level potency)?
Definition
intermediate potency classical antipsychotic
Term
perphenazine is what kind of drug (what level potency)?
Definition
intermediate, classical antipsychotic
Term
thiothixene is what kind of drug (what level potency)?
Definition
intermediate classical anitpsychotic
Term
haloperidol is what kind of drug (what level potency)?
Definition
high potency, classical anti-psychotic
Term
Fluphenazine is what kind of drug (what level potency)?
Definition
high, classical antipsychotic
Term
Sedation and hypotension seen in classical antipsychotics are due to what?
Definition
alpha 1 blockade
Term
Why is it that EPS and anticholinergic properties of a gvn classical antipsychotic are inversely related?
Definition
have anticholinergic effects in CNS protects from EPS
Term
Which class of classical antipsychotics show the greatest degree of EPS?
Definition
high potency b/c no built in anticholinergic
Term
which classical antipsychotic has the smallest degree of EPS?
Definition
Thioridazine (also has the highest anticholinergic effects)
Term
Clozapine is what kind of drug?
Definition
Atypical 2nd generation antipsychotic
Term
Olanzapine is what kind of drug?
Definition
Atypical 2nd generation antipsychotic
Term
Risperidone is what kind of drug?
Definition
Atypical 2nd generation antipsychotic
Term
What is the fatal side effect of clozapine that you have to watch out for?
Definition
agranulocytosis (1-2%)
Term
mechanism of action: atypical antipsychotics such as clozapine, risperidone, olanzapine
Definition
D1, D2, D4 blockade + anatogonism of 5HT2A receptors
Term
what differentiates the 2nd generation of antipsychotics from the 1st generation?
Definition
Produce little EPS and may be slightly more effective in tx the negative sx of schizophrenia such as apathy, emotional quieting, loss of insight, poor social interaction)
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