Antipsychotics Flashcards
The antipsychotic drugs fall into 2 major groups.. What are they?
First generation antipsychotics (FGAs)
-aka conventional antipsychotics
Second generation antipsychotics (SGAs)
-aka atpyical antipsychotics
Which group is better: FGA or SGA?
They are both equally effective
All of the FGAs produce strong blockade of receptors for ____ in the CNS. What does this result in?
Strong blockade of receptors for DOPAMINE in the CNS; this results in serious movement disorders
Extrapyramidial symptoms (EPS)
Serious movement disorders
What do the SGAs produce (like what blockade)?
Moderate blockade of receptors for dopamine; much stronger blockade of receptors for serotonin
Which has a lower risk for EPS: FGA or SGA?
SGA, since the blockade of receptors for dopamine is only moderate, whereas FGA has strong blockade of receptors for dopamine
Even thought the SGAs carry a lower risk for EPS, they cause significant risk for metabolic effects. What are some examples?
- Weight gain
- Diabetes
- Dyslipidemia
Define: A chronic psychotic illness characterized by disordered thinking and a reduced ability to comprehend reality
Schizophrenia
When do symptoms of schizophrenia usually emerge?
During adolescence or early adulthood
What are the positive symptoms of schizophrenia?
*Positive symptoms are viewed as an exaggeration or distortion of normal function
Hallucinations
Delusions
Disorganized speech
Bizarre behavior
What are the negative symptoms of schizophrenia?
*Negative symptoms can be viewed as a loss or diminution of normal function
Blunted affect
Poverty of thought
Loss of motivation
Inability to experience pleasure
Do FGAs improve positive symptoms, negative symptoms, or both?
Positive symptoms only
What are the 4 examples of FGAs?
Chlorpromazine
Haloperidol
Thiothixene
Trifuperazine
Which is more potent? Haloperidol or chlorpromazine?
Haloperidol
What does it mean when we say a drug is more potent?
The dose of the more potent drug (ex: haloperidol) required to believe psychotic symptoms is smaller than the required dose of the less potent drug (ex: chlorpromazine)
It DOES NOT mean that the more potent drug will produce greater effects.
If low potency and high potency neuroleptics (another name for FGAs) are equally effective, why do we distinguish between them?
These agents produce identical antipsychotic effects, but they differ SIGNIFICANTLY in their side effects
What is the primary indication for antipsychotic drugs?
Schizophrenia
FGA agents are equally effective, but individual patients may respond differently from one FGA to another. So how is selection on an FGA based?
It’s side effects
Do FGAs have many or few side effects?
Many
Of the many side effects that FGAs may produce, what is the most troubling?
Extrapyramidal reactions–especially tardive dyskinesia (TD)
What are 4 types of EPS?
Acute dystonia
Parkinsonism
Akathisia
Tardive dyskinesia
Three of the 4 types of EPS occurs early in therapy. What are they? Can they be managed?
Acute dystonia
Parkinsonism
Akathisia
Yes, they can be managed with a variety of drugs
*The early reactions occur LESS FREQUENTLY with LOW-POTENCY agents than with high potency agents
What is the type of EPS that occurs late in therapy? Does it have satisfactory treatment?
Tardive dyskinesia; No satisfactory treatment
*The risk of TD is equal with ALL FGAs
Describe what happens in acute dystonia
- Muscle tightening (spasms) usually of the neck and shoulders
- Can involve the tongue and eyes
- Occur early in therapy
Describe what happens in akathisia
- Literally means “can’t sit”
- A motor restlessness–> constant drive to move
- Occurs early in therapy
Describe what happens in Parkinsonism
- Exact same presentation as Parkinson’s disease (tremor, shuffling gait, decreased arm swing, and mask-like facies)
- Occurs early in therapy
Describe what happens in Tardive dyskinesia
- Means “late movement disorder”
- Occurs late in therapy
- Usually permanent
- Involuntary movement of tongue, eyes, lips, and face
If a schizophrenia patient has been on FGAs for 2 years and begins showing symptoms of involuntary movement of the tongue and eyes, what kind of EPS would she have?
Tardive dyskinesia
*Even though acute dystonia has these same characteristics, the key word of the patient having been taking the drug for 2 years already lets you know that this is TD.
Which FGA drugs are used more often: low or high potency?
High; because they produce fewer side effects
High potency FGAs causes more ____, but less ____, ____, ____.
More early EPS, but less sedation, orthostatic hypotension, and anticholinergic effects
FGA: Is haloperidol low or high potency?
High
FGA: What is haloperidol a preferred agent for?
Tourette’s syndrome
- It can also be used to control severe behavior problems in children
- It is used more than other FGAs
FGA: Haloperidol is a high potency drug. Based on what we know, what kind of effects may we see?
Early EPS; As well as: -less sedation -less orthostatic hypotension -less anticholinergic effects
FGA: Is trifluoperazine low or high potency?
High potency
FGA: is thiothixene low or high potency?
High potency
FGA: is haloperidol low or high potency?
High potency
FGA: is chlorpromazine low or high potency?
Low potency
FGA: Chlorpromazine is a low potency drug. What sort of adverse effects may be seen here?
(the opposite of a high potency drug)
- Sedation
- Orthostatic hypotension
- Anticholinergic effects
Which antipsychotic drug class is less likely to cause EPS effects, including TD?
SGAs
SGAs may have less of a risk for getting EPS, but what do SGAs carry a serious risk for?
Metabolic effects
- Weight gain
- Diabetes
- Dyslipidemia (can lead to cardiovascular events and premature death)
*Can also cause sedation, orthostatic hypotension, and can increase the risk of death when used to treat demential-related psychosis in older adults
So even though SGAs and FGAs are similar in effectiveness, which one costs 10-20x more than the other
SGAs cost 10-20x more than FGAs
What is the MOA of SGAs?
Block dopamine and serotonin
What are the 4 types of SGAs?
clozapine
rrisperidone
olanzapine
quetipine
Do SGAs treat both positive and negative effects, or only one?
They treat both!
What is the most effective SGA for schizophrenia?
clozapine
What problem does clozapine cause that makes it a drug only given to patients who have not responded to safer alternatives?
It causes agranulocytosis
What is agranulocytosis
An increased deficiency in granulocytes in the blood causing an increased vulnerability to infection
What is NMS?
Neuroleptic malignant syndrome
Is NMS more likely to occur with FGA or SGA drugs?
FGA
Is NMS more likely to occur with high or low potency FGAs?
High potency
What are the symptoms of NMS?
"lead pipe rigidity" Fever Encephalitis VS instability Elevated WBC & CPK Rigidity Sweating