Anti-Psychotics Flashcards
According to the DA hypothesis of schizophrenia, do symptoms arise due to an excess or a lack of DA in the CNS?
Excess of DA
What characterizes the positive symptoms of schizophrenia?
Hallucinations; delusions; thought disorders
What characterizes the negative symptoms of schizophrenia?
Speech disorders; flat affect; amotivation; social withdrawal
What is the MOA of “typical” antipsychotic agents?
Inhibition of D2 receptors in the mesolimbic system of brain
What is the MOA of “atypical” antipsychotic agents?
Inhibition of 5-HT2 receptors (D2 receptors still involved to some extent)
Give examples of typical antipsychotics
Haloperidol; chlorpromazine; thioridazine; fluphenazine; pimozide
Give examples of atypical antipsychotics
Clozapine; risperidone; aripiprazole; olanzapine; aiprasidone; quetiapine
Name two typical antipsychotics commonly used in the treatment of Tourette syndrome
- Haloperidol
2. Pimozide
What are Extrapyramidal symptoms (EPS)?
Parkinsonian-like symptoms (dystonia, rigidity, tremor, and bradykinesia); akathisia; tardive dyskinesia (TD)
What is akathisia?
Motor restlessness
What is Tardive Dyskinesia?
Inappropriate movements of the tongue, neck, trunk, and limbs (associated w/ long-term DA antagonist use)
What is the mechanism of antipsychotic-induced TD?
Long-term DA receptor inhibition –> upregulation & supersensitivity of DA receptors –> DA over-stimulation (especially when antipsychotic has been discontinued)
Which antipsychotics are more likely to cause EPS?
High potency typical antipsychotics such as haloperidol and fluphenazine secondary to their weak anticholinergic activity
What do thioridazine and chlorpromazine have a lower EPS potential?
They have high anticholinergic activity
What medications are used to treat antipsychotic-induced EPS?
Benztropine; amantadine; diphenhydramine (due to anticholinergic action)
How do antipsychotics cause parkinsonian-like symptoms?
Inhibition of DA receptors in the nigrotriatal pathway
How do antipsychotics cause orthostatic hypotension?
Inhibition of alpha-adrenergic receptors in vasculature
How do antipsychotics cause prolactinemia?
Inhibition of DA receptors in the anterior pituitary
Which two antipsychotics posses the highest antimuscarinic activity?
- Chlorpromazine
2. Thioridazine
Characterize the antimuscarinic activity of chlorpromazine and thioridazine
Xerostomia; blurred vision; confusion; constipation; urinary retention
Which antipsychotic agents are more effective at treating negative symptoms?
Atypical antipsychotics
Which phenothiazine antipsychotic is also used to treat intractable hiccups?
Chlorpromazine
Which phenothiazine antipsychotic may cause priapism, agranulocytosis, blue-gray discoloration of the skin, and lower seizure threshold?
Thioridazine
Which two typical antipsychotics can be formulated as depot IM injections that may last up to 3 wks?
- Haloperidol
2. Fluphenazine
Which atypical antipsychotic is usually reserved as a third-line agent to treat schizophrenic patients refractory to traditional therapy?
Clozapine
What is the major dose-limiting side effect of clozapine?
Agranulocytosis
How are patients receiving clozapine therapy monitored?
WBCs obtained @ baseline and weekly for the first 6 months of thearpy
What adverse effect is more common with clozapine, agranulocytosis, or seizures?
Seizures
Why is gynecomastia a common adverse effect of risperidone?
Risperidone induces prolactinemia (only atypical antipsychotic that significantly increases prolactin levels)
What is a potential life-threatening adverse effect of antipsychotic medications?
Neuroleptic malignant syndrome (NMS)
What characterizes NMS (Neuroleptic malignant syndrome)?
Hyperthermia; rigidity; altered mental status; CV instabiity
What is the treatment for NMS?
Dantrolene + Bromocriptine
What is the additional adverse effects of olanzapine?
Weight gain; hyperglycemia; sialorrhea
What are the additional adverse effects of quetiapine?
Hypercholesterolemia; hypertriglyceridemia; weight gain; hepatotoxicity
What is the MOA of aripiprazole?
Antagonist @ 5-HT2A receptors; partial agonist @ D2 & 5-HT1A receptors
What are the additional adverse effects of aripiprazole?
Weight gain; rash; sialorrhea; hepatotoxicity
Which antipsychotic has the highest incidence of sialorrhea?
Clozapine
