Antipsychotics Flashcards

1
Q

positive symptoms of schizophrenia

A

“presence of what shouldn’t be”:

*hallucinations
*delusions
*thought disorders

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2
Q

negative symptoms of schizophrenia

A

“lack of what should be”:

*losing interest and motivation in life and activities (e.g. relationships, sex)
*social inattentiveness
*affective flattening
*poverty of speech/content of speech
*poor self care, loss of persistence in school/work

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3
Q

typical antipsychotics - overview

A

*first generation
*effective against positive symptoms only
*more EPS
*seldom used (except haloperidol)
*MOA: D2 blockade > 5-HT2A blockade

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4
Q

atypical antipsychotics - overview

A

*second generation
*effective against positive AND negative symptoms
*less EPS
*used frequently
*MOA: 5-HT2A > D2 blockade

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5
Q

general MOA of typical antipsychotics

A

D2 blockade > 5-HT2A (serotonin) blockade

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6
Q

general MOA of atypical antipsychotics

A

5-HT2A (serotonin) blockade > D2 blockade

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7
Q

phenothiazines

A

*a class of typical antipsychotics
*example = chlorpromazine (Thorazine) (low potency)

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8
Q

butyrophenones

A

*a class of typical antipsychotics
*example = haloperidol (Haldol) (high potency)

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9
Q

chlorpromazine - drug class

A

LP phenothiazine (typical/first generation antipsychotic)

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10
Q

important atypical antipsychotics

A

*Clozapine (Clorazil)
*Risperidone (Risperdal)
*Olanzapine (Zyprexa)
*Quetiapine (Seroquel)
*Ziprasidone (Geodon)
*Aripiprazole (Ablify)
*Paliperidone (Invega)

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11
Q

clozapine - drug class

A

atypical antipsychotic

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12
Q

risperidone - drug class

A

atypical antipsychotic

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13
Q

olanzapine - drug class

A

atypical antipsychotic

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14
Q

quetiapine - drug class

A

atypical antipsychotic

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15
Q

ziprasidone - drug class

A

atypical antipsychotic

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16
Q

aripiprazole - drug class

A

atypical antipsychotic

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17
Q

paliperidone - drug class

A

atypical antipsychotic

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18
Q

pharmacokinetics/dynamics of atypical antipsychotics

A

*absorbed orally, but some have first pass metabolism (IV dose might be < PO dose)
*most have large Vd (very lipid soluble)
*hepatically metabolized (CP450)

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19
Q

mechanism for adverse drug effects of antipsychotics: loss of accommodation, dry mouth, difficulty urinating, constipation

A

*mechanism = muscarinic cholinoceptor blockade (anticholinergic effects)

*system causing the symptoms = autonomic nervous system

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20
Q

mechanism for adverse drug effects of antipsychotics: orthostatic hypotension, impotence, failure to ejaculate

A

*mechanism = alpha-adrenoceptor blockade

*system causing the symptoms: autonomic nervous system

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21
Q

mechanism for adverse drug effects of antipsychotics: Parkinson’s syndrome, akathisia, dystonias

A

*mechanism = dopamine receptor blockade

*system causing the symptoms = central nervous system

22
Q

mechanism for adverse drug effects of antipsychotics: tardive dyskinesia

A

*mechanism = supersensitivity of dopamine receptors

*system causing the symptoms = central nervous system

23
Q

mechanism for adverse drug effects of antipsychotics: toxic-confusional state

A

*mechanism = muscarinic blockade (anticholinergic effects)

*system causing the symptoms = central nervous system

24
Q

mechanism for adverse drug effects of antipsychotics: amenorrhea-galactorrhea, infertility, impotence

A

*mechanism = dopamine-receptor blockade resulting in hyperprolactinemia

*system causing the symptoms = endocrine system

25
Q

mechanism for adverse drug effects of antipsychotics: weight gain

A

*mechanism = possibly combined H1 and 5-HT2A blockade

26
Q

akithisia

A

*a subjective feeling of restlessness
*one of the extrapyramidal symptoms (EPS) associated with antipsychotics

27
Q

acute dystonic reactions

A

*abrupt onset muscular spasms of the neck, eyes, trunk, extremities
*one of the extrapyramidal symptoms (EPS) associated with antipsychotics

28
Q

parkinsonism

A

*stiffness, tremor, bradykinesia
*one of the extrapyramidal symptoms (EPS) associated with antipsychotics

29
Q

extrapyramidal symptoms

A

*akithisia (restless/can’t sit still)
*acute dystonic reactions
*parkinsonism

30
Q

cause of extrapyramidal symptoms (EPS)

A

*associated with use of antipsychotics
*highest incidence with high potency typical agents (haloperidol)

31
Q

MOA of extrapyramidal symptoms (EPS)

A

*D2 blockade + imbalance with M1 (Ach)

32
Q

treatment for extrapyramidal symptoms (EPS)

A

*treat with ANTICHOLINERGIC drug
-benztropine
-trihexyphenidyl
-diphenhydramine**

*do NOT give levodopa

33
Q

tardive dyskinesia (TD)

A

*a horrible adverse drug effect associated with antipsychotics
*late-occurring abnormal movements:
-mouth and tongue movements (lip smacking, sucking and puckering, facial grimacing)
-irregular movements of the limbs (choreoathetoid-like movements of the fingers and toes; slow, writing movements of the trunk)
*relative cholinergic deficiency secondary to SUPERSENSITIVITY OF DOPAMINE RECEPTORS

34
Q

MOA of tardive dyskinesia

A

*relative cholinergic deficiency secondary to supersensitivity of DA receptors
*occurs after long-term use with antipsychotics (esp typicals)

35
Q

tardive dyskinesia - treatment

A

*discontinue the drug (switch to newer atypical agent)
*can try high dose benzos
*VMAT inhibitors (block the uptake of dopamine into synaptic vesicles)

36
Q

neuroleptic malignant syndrome (NMS)

A

*ADE associated with antipsychotics
*fever, rigidity, mental status changes, and autonomic instability
*from DA blockade
*TX: bromocriptine (DA agonist); DANTROLENE (a muscle relaxant)

37
Q

treatment for neuroleptic malignant syndrome (NMS)

A

*bromocriptine (DA agonist)
*dantrolene (a muscle relaxant)

38
Q

other neurologic ADEs of antipsychotics

A

*seizures (decreases seizure threshold) - esp with clozapine
*sedation (from central histamine-1 blockade)

39
Q

hyperprolactinemia

A

*ADE of antipsychotics
*s/s: sexual dysfunction (decreased libido, infertility, impotence), amenorrhea, gynecomastia / galactorrhea, hypoestrogenism / osteopenia

40
Q

general drugs that cause hyperprolactinemia

A

*all typical antipsychotics
*risperidone
*paliperidone

41
Q

cardiovascular effects associated with antipsychotics

A

*alpha-1 blockade: orthostatic hypotension (reflex tachycardia) & impaired ejaculation
*QTc prolongation (be careful adding to other QTc drugs)

42
Q

metabolic effects associated with antipsychotics

A

*weight gain
*diabetes mellitus
*dyslipidemia

43
Q

ADEs of clozapine

A

*agranulocytosis
*myocarditis

(note - minimal EPS)

44
Q

clozapine - unique facts

A

*minimal EPS and high efficacy
*causes AGRANULOCYTOSIS & MYOCARDITIS
**REQUIRES A SPECIAL PROGRAM (REMS) dictating who can prescribe it and frequency of CBC monitoring

45
Q

ADEs of aripiprazole - general

A

probably the LEAST ADEs of all of the antipsychotics (used alot)

46
Q

ADEs of clozapine - general

A

probably the MOST ADEs of all of the atypical antipsychotics (worst tolerated)

47
Q

ADEs of olanzipine

A

*metabolic ADEs - weight gain, glucose abnormalities, and hyperlipidemia

48
Q

ADEs of ziprasidone

A

*QTc prolongation

49
Q

prochlorperazine

A

*antiemetic (treat nausea and vomiting)
*MOA: DA-receptor blockade in the chemoreceptor trigger zone and in stomach
*has high-potency ADEs (especially extrapyramidal symptoms - EPS)

50
Q

promethazine

A

*antiemetic (treats nausea and vomiting)
*MOA: DA-receptor blockade in the chemoreceptor trigger zone and in stomach
*ADE = sedation (potent histamine-1 blocking effects)

51
Q

antipsychotic drug used for acute agitation

A

haloperidol

52
Q

drugs used for nausea and vomiting

A

*prochlorperazine
*promethazine