CNS III- Neuroleptic (Antipsychotic) Drugs Flashcards
What is the primary use of antipsychotic drugs?
Treatment of schizophrenia
What are some of the clinical symptoms of schizophrenia?
Positive (psychotic) symptoms - delerium, paranoia, hallucinations (auditory most common)
Cognitive dysfunction - working memory, attention, executive function (abstract thinking, problem solving)
Negative symptoms - apathy, withdrawl, anhedonia (lack of pleasure)
First generation anti-psychotic drugs are not as effective as treating what kind of symptoms?
Negative symptoms
What are some adverse effects of 1st gen antipsychotic drugs?
-Extra Pyramidal Syndrome (EPS) effects
parkinsonism, dystonia, akathisia (involuntary movements)
-Tardive dyskinesia (severe)-tx with tetrabenzine
-Sexual Dysfunction
-Hypotension
-Hyperprolactinemia-tx with bromocryptine
-Neuroleptic malignant syndrome
What is neuroleptic malignant syndrome defined by?
- Rare, 0.2 to 3% incidence (2:1, ♂:♀)
- Life-threatening neurological disorder, 10% mortality rate
- Muscle rigidity, cramps, tremors
- Fever (malignant hyperthermia)
- Autonomic instability (unstable BP, hypertensive crisis)
- Cognitive changes (confusion, delirium, agitation, coma)
- Elevated serum creatine kinase and white blood cell counts,
- Rhabdomyolysis, sometimes myoglobinemia,
- Catatonia, stupor
- Diaphoresis (excessive sweating)
FEVER and FALTER mnemonics for neuroleptic malignant syndrome
FEVER F – Fever E – Encephalopathy V – Vitals unstable E – Elevated enzymes (CPK) R – Rigidity of muscles
FALTER F – Fever A – Autonomic instability L – Leukocytosis T – Tremor E – Elevated enzymes (elevated CPK) R – Rigidity of muscles
Which atypical neuroleptic requires monitoring with weekly blood tests?
Clozapine- there is approximately a 1% incidence of agranulocytosis while taking this drug (can be lethal)
Which neuroleptic drug(s) is associated with increased risk of seizures?
Clozapine, chlorpromazine
Name the class that the following drugs fall into: Chlorpromazine, Fluphenazine, Trifluoperazine, Perphenazine, Thioridazine, Thiothizene, Loxapine, Haloperidol
First generation antipsychotics
What is the mechanism of all of the first generation antipsychotics? (Chlorpromazine, Fluphenazine, Trifluoperazine, Perphenazine, Thioridazine, Thiothizene, Loxapine, Haloperidol)
D2 receptor antagonist
Which two first generation antipsychotics generate more EPS than Chlorpromazine? Less?
More-Haloperidol and Fluphenazine
Less- Perphenazine, and Loxapine
What is meant by saying that the first generation antipsychotics produce an “artificial hibernation”?
These drugs induce catalepsy (trance, muscle rigidity, lack of voluntary movement)
What is the mechanism of action tetrabenazine and what is it used to treat?
Depletes dopamine, inhibits VMAT2 (transporter for repackaging monoamines)
Treats-movement disorder in Huntingtons and tardive dyskinesias
What is the mechanism of action of Dantrolene and what is it used to treat?
muscle relaxant to treat malignant hyperthermia in NMS
What are the 7 second generation antispsychotics?
Clozapine, Olanzapine, Quetiapine, Risperidone, Ziprazidone, Paliperidone (metabolite of risperidone) and Aripiprazole
What is the mechanism of action of the 2nd generation antipsychotics excluding Aripiprazole?
D2 and 5HT2 receptor antagonism
Which of the following may have limited use due to Agranulocytosis and must be monitored by weekly blood tests? Clozapine, Olanzapine, Quetiapine, Risperidone, Ziprazidone, Paliperidone
Clozapine-also has seizure risk, Akathesia, GI hypomotility and myocarditics
Which of the following drugs has a higher incidence of cardiac arrythmias from QT prolongation? Clozapine, Olanzapine, Quetiapine, Risperidone, Ziprazidone, Paliperidone
Ziprazidone, and Paliperidone
What are some of the common side effects of almost all second generation antipsychotics?
weight gain, hyperglycemia, postural hypotension, somnolence (except risperidone and paliperdone-insomnia) and constipation
What are the side effects of Ziprazidone and Paliperidone in addition to the side effects of other 2nd generation antipsychotics?
QT prolongation, insomnia, hyperprolactinemia, dizziness, EPS
Which of the following may increase serum hepatic transaminases? Clozapine, Olanzapine, Quetiapine, Risperidone, Ziprazidone, Paliperidone
Olanzapine
Which of the second generation antipsychotics has less metabolic complications?
Risperidone, Ziprazidone, and Paliperidone (non-tricyclics)
What is the mechanism of action of Aripiprazole?
- partial D2, D3 and 5HT1a receptor agonist
- 5HT2a antagonist
What is Aripiprazole used to treat?
Schizophrenia-not as effective as other atypicals
Bipolar
Depression-as adjunct
