Antipsychotic Drugs Flashcards
Name the typical antipscyhcotics
Chlorpromazine Fluphenazine Perphenazine Thiothixene Haloperidol
Name the atypical antipsychotics
Clozapine Risperidone Olanzapine Quetiapine Ziprasidone Aripiprazole Paliperidone Lurasidone Asenapine
What is alogia?
Lack of speech
What is avolition?
Lack of initiative (motivation)
Which Dopamine receptors inhibit Adenylate Cyclase?
D2, D3, D4
Which Dopamine receptors activate Adenylate Cyclase?
D1 and D5
What does Adenylate Cyclase do?
converts ATP to cAMP
What is the MoA of typical antipsychotics?
Dopamine D2 blockers
What type of symptoms are typicals good for treating?
Postive Symptoms
Which Dopamine receptors inhibit Adenylate Cyclase?
D2, D3, D4
Which Dopamine receptors activate Adenylate Cyclase?
D1 and D5
What is the relevance of high potency typicals? Why do they do this?
High potency have higher chance of EPS, and they offer less sedation. This is due to weak anticholinergic effect and autonomic SAs.
What is the MoA of typical antipsychotics?
Dopamine D2 blockers
What type of symptoms are typicals good for treating?
Postive Symptoms
What is the rank of potency of typicals?
Haloperidol>Fluphenazine=Perphenazine>Thiothixene>Chlorpromazine
What is the relevance of low potency typical? Why do they do this?
Low potency typicals have lower incidence of Extra Pyramidal Symptoms (EPS). This is because of their antimuscarinic effects
What is the relevance of high potency typicals? Why do they do this?
High potency have higher chance of EPS, and they offer less sedation. This is due to weak anticholinergic effect and autonomic SAs.
What type of symptoms are atypicals good for treating?
Negative Symptoms
What is the potency of Clozapine?
Low potency
What is the MoA of Risperidone?
5-HT2/D2 agonist
What is the only approved antipsychotic for children and teens?
Risperidone
What is the primary active metabolite of Risperidone?
Paliperidone
What is the MoA of Aripiprazole?
D2 partial agonist
5-HT2A antagonist, 5-HT1A partial agonist
What is the MoA of Ziprasidone?
5-HT2A, 5-HT1A, 5-HT2C/D2 antagonist
Which atypical antipsychotic acts as a D1, D2, 5-HT1, 5-HT2, alpha adrenergic and histamine receptor antagonist. With low affinity for muscarinic receptors?
Asenapine
What is the MoA of Lurasidone?
D2 and 5-HT2A antagonist
Partial agonist of 5-HT1A
Which atypical antipsychotic has the highest incidence of EPS?
Lurasidone
What effects do antipsychotics have in the Cerebral Cortex?
They can lower the threshold for seizures. This most often occurs with low potency drugs like the phenothiazines (Chlorpromazine, Fluphenazine, and Perphenazine)
What effects do antipsychotics have in the Basal Ganglia?
Decrease dopamine activity. This causes EPS.
Initially, they increase dopamine metabolism, synthesis, and firing rate, but this diminishes over time.
At what site in the brain do antipsychotics have their antipsychotic effect?
Limbic System
Which antipsychotic is an antidiuretic?
Chlorpromazine
Which antipsychotics have the most increase in prolactin secretion?
All Typicals and Risperidone
Which antipsychotics have no increase or decrease Prolactin secretion?
Quetiapine
Aripiprazole (may decrease secretion)
What effects do antipsychotics have in the brain stem at low doses?
Decreased vasomotor reflexes
What effects do antipsychotics have in the chemoreceptor trigger zone in low doses?
anti-nausea and vomiting elicited by activation of dopamine receptors
Which antipsychotic is an antidiuretic?
Chlorpromazine
What are the SAs of Chlorpromazine?
antidiuretic lowers glucose tolerance lowers insulin release orthostatic hypotension causes jaundice Urticaria in 5% of patients
Which atypical antipsychotics increase the risk of DM2?
Atypicals: Clozapine and Olanzepine have highest risk
Which atypical antipsychotics have the least risk of DM2
Aripiprazole and Ziprasidone
Which EPS symptoms have the latest onset?
Perioral Tremor
Tardative Dyskinesia
Which atypical antipsychotics have the least incidence of weight gain?
Ziprasidone (+/-) and Aripiprazole (+)
Which atypical antipsychotic has the highest risk of causing EPS?
Risperidone
Which atypical antipsychotics have the highest potential for CYP interactions?
Aripiprazole
Quietipine
Respiridone
Ziprasidone
In a patient who develops Parkinsonian syndrome due to antipsychotic Rx, which two medications are contraindicated to treat this new problem? Why?
L-DOPA and Bromocriptine are contraindicated because they can induce agitation and enhance the psychosis
Which EPS symptoms have a delayed onset?
Perioral Tremor
Tardative Dyskinesia
Which EPS symptom can appear within the first 5 days of therapy?
Acute Dystonia
Which EPS symptom can develop within 5-60 days of therapy?
Akathesia (There’s ants in my pants!!!)
Which EPS symptom can develop within 5-30 days of therapy?
Parkinsonian syndrome
In a patient who develops Parkinsonian syndrome due to antipsychotic Rx, which two medications are contraindicated to treat this new problem? Why?
L-DOPA and Bromocriptine are contraindicated because they can induce agitation and enhance the psychosis
What are the symptoms of Neuroleptic Malignant Syndrome?
Fever Severe Parkinsonism with catatonia Fluctuations in coarse tremor intensity Autonomic instability high creatine kinase Myoglobinemia
What is the mortality rate in NMS?
High (10%)
How do you treat NMS?
STOP the antipsychotic
Dantrolene (muscle relaxant) or bromocriptine
Which drug will require weekly white blood cell counts? Why?
Clozapine
Because this can cause agranulocytosis (can see leukopenia before onset)
Which atypical antipsychotics have the highest incidence of metabolic syndrome?
Olanzapine
Which atypical antipsychotics have the lowest risk of metabolic syndrome?
Zisprasidone and Aripiprazole
Which side effect is caused seretonergic, muscarinic, noradrenergic, and D2 blockade?
Sexual side effects
What type of tissues do antipsychotics accumulate in?
High blood supply tissues
Should a pregnant woman take antipsychotics? Why?
Probably not.
Crosses placental barrier and enters beast milk.
Which antipsychotics have active metabolites?
Chlorpromazine
Phenothiazines (chlorpromazine, Fluphenazine, Perphenazine)
Respiridone (*Paliperidone)
Aripiprazole
Name the long acting depot antipsychotics
Prolixin Decanoate
Haldol Decanoate
Risperidal Consta
What are some miscellaneous uses of antipsychotics?
Nausea and Vomiting (low dose)
Alcoholic hallucinosis
Neuropsychiatric disease with movement disorders: Tourette’s , Huntington’s, Intractable Hiccup
