CNS 3 - Neuroleptic Flashcards
What are the 5 phenothiazines (typical antipsychotics)? What are their limitations to treating schizophrenia or mania?
Chlorpromazine, thioridazine, fluphenazine, perphenazine, trifluoperazine
- little effect on negative symptoms, EPS side effects, development of TD in long term use, hyperprolactinemia
How do phenothiazines work?
-D2 receptor antagonist: induce catalepsy (trance, muscle rigidity, lack of voluntary movement)
What is an important side effect of all of the first generation antipsychotics, and what clinical features can be seen?
Neuroleptic malignant syndrome - sudden reduction of dopamine activity
- autonomic instability
- cognitive changes
- elevated CK, WBCs
- fever
What drugs possess a high risk of producing NMS?
haloperidol and chlorpromazine or an abrupt withdrawal of levodopa in PD patient
What are three typical antipsychotics (1st gen) that do not fit into the class of phenothiazines?
- thiothixene, loxapine, and haloperidol
- carry same other characteristics and risk factors
On psych rotation, you meet a patient that is experiencing hallucinations that have not improved with typical antipsychotics. You decide to start clozapine. How does this drug work and what is an important dangerous side effect you should be on the look out for?
Clozapine antagonizes the D2 and 5HT2 receptors
- important SE is agranulocytosis!
- also possible is weight gain, akathesia
Which 2nd generation antipsychotic is associated with fewer metabolic complications than the others?
ziprazidone
Which 2nd gen antipsychotic has the greatest tendency to produce EPS?
risperidone
Why is dosing antipsychotics so tricky?
Small window between effective antipsychotic mechanism (striatal D2 receptor occupancy) and the development of EPS
Which dopamine pathway causes (+) symptoms and which causes (-) symptoms?
- mesolimbic and mesocortical, respectively
Activity at what receptor causes the side effects of weight gain and sedation that can be seen with many antipsychotics?
H1
How does aripiprazole work and what can it be used for?
- partial D2 & D3 receptor agonist
- partial 5HT1a agonist
- 5HT2a antagonist
- can be used to treat bipolar or as an adjunct in depression
Olazapine, an atypical antipsychotic, produces very little EPS, TD, and no agranulocytosis. What is its main drawback to use?
- metabolic complications
Which antipsychotics can be used in a pregnant patient?
- clozapine and lurasidone
You suspect NMS in a patient that you just started on haloperidol. What do you do?
- stop haloperidol!
- administer bromocriptine to replenish DA
- administer dantrolene if malignant hyperthermia is an issue
