Antipsychotics

Question 1

What are the positive symptoms of schizophrenia (3)?

Answer 1

hallucinations, delusions, aggressive behaviors

Question 2

What are the negative symptoms of schizophrenia (2)?

Answer 2

lack of speech or emotion expression, social withdrawal

Question 3

What are the cognitive symptoms of schizophrenia (2)?

Answer 3

difficulties with concentration and memory, executive decision making abilities

Question 4

what are some bad things about schizophrenia?

Answer 4

high suicide risk, homeless, non-compliance, expensive treatment

Question 5

What are the two classifications of typical antipsychotics?

Answer 5

phenothiazines, butyrophenones

Question 6

What is the phenothiazine?

Answer 6

Chlorpromazine

Question 7

What is the butyrophenones?

Answer 7

Haloperidol

Question 8

Which was the first antipsychotic?

Answer 8

Chlorpromazine

Question 9

What are two characteristics of Chlorpromazine?

Answer 9

it preferentially treats psychotic sxs (esp. positive symptoms) while leaving pts relatively conscioius, it’s more sedating than newer atypical antipsychotic drugs

Question 10

What is the mechanism of action of typical antipsychotics?

Answer 10

block dopamine receptors, especially D2

Question 11

What is the dopamine hypothesis?

Answer 11

1) both amphetamine and cocain block reuptake of DA and foster psychotic symptoms
2) antipsychotics block DA D2 receptors

Question 12

Which DA receptors do typical antipsychotics antagonize?

Answer 12

D2!

Question 13

What other receptors do typical antipsychotic drugs have affinities for?

Answer 13

HAMS: Histamine, a1 Adrenergic, Muscarinic, Serotonin (5HT). each drug has a iunique binding profile

Question 14

What are two problems with typical antipsychotics?

Answer 14

1) persistent sxs in ~30% patients (treatment refractory)

2) only modest improvement of negative and cognitive sxs

Question 15

What are the side effects of typical antipsychotics?

Answer 15

extrapyramidal symptoms (EPS - parkinsonism) due to D2 receptor blockade in the nigrostriatal pathway, hyperprolactemia due to D2 blockade in the tuberoinfundibular system

Question 16

What defines the atypical antipsychotics?

Answer 16

reduced tendency to cause EPS and hyperprolactinemia

Question 17

What are the two characteristics of the atypical antipsychs?

Answer 17

relatively weak D2 dopamine receptor blocking acitvity, Serotonin 2A (h-HT2A) receptor antagonism

Question 18

does 5-HT@A antagonism affect antipsychotic effects?

Answer 18

no because inhibition of DA release by serotonin is not as prominent in mesocoritcal/mesolimbic pathways

Question 19

which dopamine pathways do relief of psychosis happen?

Answer 19

mesolimbic (positive symptoms) and mesocortical (negative symptoms?)

Question 20

true or false: each atypical agent has a unique receptor blocking profile

Answer 20

true

Question 21

what syndrome is more common with atypical antipsychotics?

Answer 21

metabolic syndrome

Question 22

What are the atypical antipsychotics?

Answer 22

clozapine, olanzapine, quetiapine, resperidone, ziprasidone, aripiprazole

Question 23

What is selection of antipsychotics based on?

Answer 23

less on therapeutic expectancy, e.g. positive or negative symptoms, really based on anticipated side effects

Question 24

What do the different side effects of antipsychotics depend on?

Answer 24

their potencies at other non-dopamine receptors

Question 25

What else are antipsychs indicated for (5)?

Answer 25

schizoaffective disorder, manic pahse of bipolar disorder, Tourette's syndrome, Huntington's disease, autistic disorders

Question 26

Which drugs cause weight gain as a side effect?

Answer 26

clozapine, olanzapine

Question 27

which drug causes sedation?

Answer 27

chlorpromazine

Question 28

What are the three extrapyramidal symptoms (EPS)?

Answer 28

Parkinsonism, tardive dyskinesia, neuroleptic malignant syndrome

Question 29

3 points about Parkinsonism?

Answer 29

1) identical sxs as parkinson's disease 2) treated with ant-muscarinic drugs (benztropine) 3) L-DOPA should never be used!

Question 30

What is tardive dyskinesia?

Answer 30

sterotyped, repetitive involuntary movements of face, eyelids, mouth, tongue, extremities, trunk

Question 31

what is often the most important problem associated with long term antipsychotic use and can be irreversible in adults?

Answer 31

tardive dyskinesia

Question 32

is there treatment for tardice dyskinesia?

Answer 32

no

Question 33

what is neuroleptic malignant syndrome?

Answer 33

life-threatening marked muscle rigidity, fever, autonomic instability, leukocystosis believed to result from excessively rapid blockade of postsynaptic dopamine receptors

Question 34

what is the treatment for neuroleptic malignant syndrome?

Answer 34

immediate discontinuation of antipsychotics, Dopamine receptor agonist )bromocriptine) and muscle relaxant (diazepam)

Question 35

What is Chlorpromazine?

Answer 35

prototype neuoleptic, inexpensive. many side effects, especially autonomic, because of relatively high muscarinic and a1 adrenergic receptor blocking activity. highly sedative. a1=5HT@A>D2>D1

Question 36

What is haloperidol?

Answer 36

inexpensive, potent, relatively clean drug with fewer autonomic effects. severe EPS and hyperprolactinemia. D2>a1>D4>5HT2A>Da>H1

Question 37

What is Clozapine?

Answer 37

less likely to cause EPS. most efficacious. agranulocytosis (dec. WBC): life threatening. other side effects: weight gain, sedation, hyperlipidemia, lowering seizure threshold. only used for patients resistant to typical antipsychotics. strict blood monitoring is mandatory.

Question 38

What is Olanzapine?

Answer 38

olanzapine and risperidone are widely regarded as the second most effective atypical antipsych drugs next to clozapine. relatively strong histamine receptor H1 antagonism. side effects: sedation, metabolic syndrome, lowering seizure threshold.

Question 39

What is Quetiapine?

Answer 39

structurally similar to clozapine. strong histamine H1 receptor antagonism (sedation, weight gain)

Question 40

What is Risperidone?

Answer 40

most potent D2 receptor blocker among atypical antipsychs (associated with EPS and hyperprolactinemia at higher dose). much less potent anti-muscarinic activity

Question 41

What is Ziprasidone?

Answer 41

low affinity for muscarinic, a1 and H1 receptors (less sedation, less postural hypotension, less weight gain). prolongs QTc interval (not indicated for patients with heart problems)

Question 42

What is Aripiprazole?

Answer 42

partial agonist for D2: high affinity for D2 receptors but only has 3-% of intrinsic activity of DA. 5-HT2A receptor antagonist. minimally sedating.

Question 43

What is the 1st antipsychotic, sedative?

Answer 43

chlorpromazine

Question 44

What is the d2 receptor antagonist?

Answer 44

haloperidol

Question 45

what is the d2 receptor partial agonist?

Answer 45

aripiprazole

Question 46

what causes prolongation of QTc interval?

Answer 46

ziprasidone

Question 47

what causes agranulocytosis?

Answer 47

cloazapine

Question 48

what is potent d2 blocking atypical?

Answer 48

risperidone

Question 49

what drug is most widely used; metabolic syndrome?

Answer 49

olanzapine