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Pharmacology Test 4 > Antipsychotics > Flashcards

Antipsychotics Flashcards

1
Q

What are the positive symptoms of schizophrenia (3)?

A

hallucinations, delusions, aggressive behaviors

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2
Q

What are the negative symptoms of schizophrenia (2)?

A

lack of speech or emotion expression, social withdrawal

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3
Q

What are the cognitive symptoms of schizophrenia (2)?

A

difficulties with concentration and memory, executive decision making abilities

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4
Q

what are some bad things about schizophrenia?

A

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

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5
Q

What are the two classifications of typical antipsychotics?

A

phenothiazines, butyrophenones

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6
Q

What is the phenothiazine?

A

Chlorpromazine

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7
Q

What is the butyrophenones?

A

Haloperidol

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8
Q

Which was the first antipsychotic?

A

Chlorpromazine

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9
Q

What are two characteristics of Chlorpromazine?

A

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

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10
Q

What is the mechanism of action of typical antipsychotics?

A

block dopamine receptors, especially D2

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11
Q

What is the dopamine hypothesis?

A

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

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12
Q

Which DA receptors do typical antipsychotics antagonize?

A

D2!

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13
Q

What other receptors do typical antipsychotic drugs have affinities for?

A

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

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14
Q

What are two problems with typical antipsychotics?

A

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

2) only modest improvement of negative and cognitive sxs

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15
Q

What are the side effects of typical antipsychotics?

A

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

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16
Q

What defines the atypical antipsychotics?

A

reduced tendency to cause EPS and hyperprolactinemia

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17
Q

What are the two characteristics of the atypical antipsychs?

A

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

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18
Q

does 5-HT@A antagonism affect antipsychotic effects?

A

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

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19
Q

which dopamine pathways do relief of psychosis happen?

A

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

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20
Q

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

A

true

21
Q

what syndrome is more common with atypical antipsychotics?

A

metabolic syndrome

22
Q

What are the atypical antipsychotics?

A

clozapine, olanzapine, quetiapine, resperidone, ziprasidone, aripiprazole

23
Q

What is selection of antipsychotics based on?

A

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

24
Q

What do the different side effects of antipsychotics depend on?

A

their potencies at other non-dopamine receptors

25
Q

What else are antipsychs indicated for (5)?

A

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

26
Q

Which drugs cause weight gain as a side effect?

A

clozapine, olanzapine

27
Q

which drug causes sedation?

A

chlorpromazine

28
Q

What are the three extrapyramidal symptoms (EPS)?

A

Parkinsonism, tardive dyskinesia, neuroleptic malignant syndrome

29
Q

3 points about Parkinsonism?

A

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

30
Q

What is tardive dyskinesia?

A

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

31
Q

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

A

tardive dyskinesia

32
Q

is there treatment for tardice dyskinesia?

A

no

33
Q

what is neuroleptic malignant syndrome?

A

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

34
Q

what is the treatment for neuroleptic malignant syndrome?

A

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

35
Q

What is Chlorpromazine?

A

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

36
Q

What is haloperidol?

A

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

37
Q

What is Clozapine?

A

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.

38
Q

What is Olanzapine?

A

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.

39
Q

What is Quetiapine?

A

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

40
Q

What is Risperidone?

A

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

41
Q

What is Ziprasidone?

A

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)

42
Q

What is Aripiprazole?

A

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

43
Q

What is the 1st antipsychotic, sedative?

A

chlorpromazine

44
Q

What is the d2 receptor antagonist?

A

haloperidol

45
Q

what is the d2 receptor partial agonist?

A

aripiprazole

46
Q

what causes prolongation of QTc interval?

A

ziprasidone

47
Q

what causes agranulocytosis?

A

cloazapine

48
Q

what is potent d2 blocking atypical?

A

risperidone

49
Q

what drug is most widely used; metabolic syndrome?

A

olanzapine

Pharmacology Test 4 (10 decks)

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