antipsychotics Flashcards

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1
Q

describe the biological basis for antipsychotic treatments?

A

involves the hyperactivation of the dopamine system

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2
Q

typical antipsychotics block which receptors?

A

d2 receptors (AC-inhibited)ari

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3
Q

the typical antipsychotics are largely effective for which type of symptoms?

A

positive symptoms

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4
Q

which type of antipsychotics causes elevated prolactin levels and also produces extrapyramidal symptoms?

A

typical antipsychotics

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5
Q

________antipsychotics are equally effective but differ in potency/side effects

A

typical

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6
Q

atypical antipsychotics block D2 receptors and what other receptors which may reduce the EPS and improve efficacy for negative symptoms?

A

5HT2A

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7
Q

which phenothiazine (low potency typical antipsychotic) has an aliphatic side chain?

A

chlorpromazine

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8
Q

What is important to remember about the typical antipsychotics that have a piperazine group in the side chain?

A

they are POTENT-fluphenazine

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9
Q

low potency typical anti-psychotics have a ______ risk of EPS , but an increased risk of antimuscarinic AEs

A

decreased

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10
Q

name the antipsychotic that has high potency and is a butyrophenone

A

haloperidol

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11
Q

which antipsychotic is only considered atypical at low doses, but is typical at high doses?

A

risperidone (5-HT2/D2 antagonist

limited EPS at low doses

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12
Q

name the only approved antipsycotic agent used in children and teens?

A

risperidone

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13
Q

name the atypical antipsychotics? (6)

A
Aripiprazole
Clozapine
Olanzapine
Quetiapine
Risperidone
Ziprasadone
"Atypicals can Occasionally quiet risky zebras"
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14
Q

which atypical antipsychotic is a D2 partial agonist that reduces actions of the full agonist?

A

aripiprazole (abilify)

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15
Q

which atypical antipsychotic has 5-HT2A antagonist and 5-HT1A partial agonist activity and has lower incidence of side effects?

A

aripiprazole (abilify)

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16
Q

name the atypical antipsychotic: 5-HT2A, H-HT1A, 5-HT2C/D2 antagonist with limited extrapyramidal symptoms

A

ziprasidone

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17
Q

name the 4 atypical antipsychotics (2nd gen.) with the highest potential for CYP interactions via CYP3A4/2D6

A
Aripiprazole
Quetiapine
Risperidone
Ziprasidone
"1, 4, 5, 6"
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18
Q

which 2 atypical antipsychotics have a high risk of causing diabetes and causing weight gain?

A

Clozapine
Olanzapine

“Cheetos & Oreos”

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19
Q

among the atypical antipsychotic drugs, which has the highest risk for EPS?

A

risperidone

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20
Q

which two atypical antipsychotics have highest for elevated prolactin level?

A

Risperidone

“PRolactin”

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21
Q

among the atypical antipsychotics, which has the highest risk for QT prolongation?

A

ziprasidone

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22
Q

what exactly are extra-pyramidal symptoms?

A

dystonias (sustained contraction of muscles leading to twisted, distorted postures)
parkinson-like symptoms
akathisia (motor restlessness)
tardive dyskinesia

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23
Q

what is neuroleptic syndrome?

A

suppression of spontaneous movements & complex behaviors
reduced initiative & interest in environment
decreased manifestations of emotions
psychotic symptoms disappear over time

24
Q

which antipsychotics can lower seizure thresholds via CNS effects?

A

low potency phenothiazines (chlorpromazine)

25
Q

why should you avoid antipsychotics in pts with established breast carcinoma?

A

antipsychotics ( risperidone) can cause increased prolactin secretion

26
Q

what part of the brain is thought to be the site of antipsychotic effects?

A

limbic system

27
Q

what class of drugs can decrease the extra-pyramidal side-effects without impacting the therapeutic effects on psychosis?

A

anticholinergics

28
Q

what are some of the clinical consequences of sustained hyperprolactinemia?

A

sexual dysfunction
amenorrhea
gynecomastia/galactorrhea

29
Q

what effects do antipsychotics have on the brainstem?

A

decreased vasomotor reflexes at low doses

30
Q

what effects do antipsychotics have on CTZ ?

A

protects against N/V elicited by activation of dopamine receptors

31
Q

which typical antipsychotic impairs glucose tolerance and decreases insulin release?

A

chlorpromazine

32
Q

how would you treat the AE of acute dystonia in a pt who was taking antipsychotic meds?

A

treat symptoms (facial grimacing, stiff neck, oculogyric crisis) with anticholinergic antiparkinsonian agents

33
Q

how do you treat the AE of akathesia (ants in the pants) from antipsychotic therapy?

A

decrease the dose of antipsychotic agent
add antiparkinsonian agent
antianxiety agent or propanolol

34
Q

how do you treat the AE of parkinsonian syndrome with antipsychotic therapy?

A

treat with anticholinergic antiparkinsonian agents or amantadine

35
Q

what is neuroleptic malignant syndrome?

A

extrapyramidal side effect w/ fever, severe parkinsonism w/ catatonia, fluctuations in coarse tremor intensity, autonomic instability
elevated creatine kinase
myoglobinemia
high mortality (10%)

36
Q

how do you treat neuroleptic malignant syndrome?

A

immediate cessation of antipsychotic
supportive care
dantroline or bromocriptine may help

37
Q

how do you treat the perioral tremor (rabbit syndrome) caused by antipsychotic meds?

A

treat with anticholinergics

38
Q

what is tardive dyskinesia and how long does it take to develop?

A

stereotyped, repetitive, choreiform movements of face, eyelids, mouth, tongue

This takes months or yrs to develop

39
Q

how long does perioral tremor take to develop?

A

months or yrs

40
Q

how do you treat tardive dyskinesia?

A

discontinue antipsychotic

41
Q

jaundice can happen during the 2nd-4th week with what antipsychotic?

A

chlorpromazine

  • hypersensitivity reaction
  • mild
  • change drugs
42
Q

blood dyscrasias (leukocytosis, leukopenia, eosinophilia) are especially important when using which antipsychotic?

A

clozapine
“watch clozapine closely”
like weekly CBCs

43
Q

Leukopenia with clozapine may be a forewarning of impending what?

A

agranulocytosis

44
Q

The bioavailability of antipsychotics increases 4-10xs when given via what route?

A

intramuscularly

45
Q

what are the exceptions to the rule that most antipsychotics have inactive metabolites?

A

7-OH-chlorpromazine
Several N-methylated metabolites of phenothiazines
Dehydroaripirazole

46
Q

describe the PKs of antipsychotics?

A

highly lipophilic
highly protein bound
accumulates in high blood supply tissues
crosses placental barrier and enters breast milk

47
Q

are most metabolites of antipsychotics inactive or active?

A

inactive

48
Q

typical antipsychotics are metabolized with which CYPs?

A

CYP2D6/3A4

49
Q

Many antipsychotics can inhibit CYP2D6, what are the effects of this?

A

can raise levels of many TCAs & SSRIs

Raise levels of many other antipsychotics

50
Q

what classes of drugs treat schizophrenia?

A

antipsychotics

51
Q

what classes of drugs treats bipolar disorder with psychotic features?

A

mood stabilizers &/or antidepressants

52
Q

what is the treatment for major depressive disorder with psychotic features?

A

ECT &/or antidepressant meds &/or antipsychotics

53
Q

what is the treatment for psychosis due to substance abuse intoxication/withdrawal?

A

definitive treatment of substance abuse condition

antipsychotics as an adjunct for delirium

54
Q

describe how the long acting depot antipsychotics have slow release?

A

have slow release of the active drug produced by combining the base AP with a fatty acid (decanoic acid)

55
Q

what happens to the alcohol group of the antipsychotic drug when used in long acting depots?

A

alcohol group is esterified by the acid producing a lipophilic compound with increased solubility in oil-usually sesame

56
Q

when should you consider using a depot prep. for antipsychotic therapy?

A

pts with several relapses who don’t take oral meds
pts who have clear cut compliance issues
when oral absorption is poor

57
Q

which typical antipsychotics can cause increased prolactin secretion?

A

ALL OF THEM