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Psychiatry > anti-psychotic drugs > Flashcards

anti-psychotic drugs Flashcards

1
Q

which receptors are blocked primarily by typical antipsychotic drugs?

A

D2

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2
Q

t/f. muscarinic, alpha-adrenergic,histamine H1 and serotonin 5-HT2 receptors are blocked by anti-psychotics agents

A

true

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3
Q

have the following characteristics:

Low D2 affinity

High 5-HT2 affinity

A

atypical antipsychotics

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4
Q

what is defined below:

Personality is seriously disorganized
 Contact with reality is usually impaired
 Ability to think, perceive, and judge is impaired (often with delusions and/or hallucinations)
 Ability to communicate and relate to others is impaired
 Ability to cope with the environment is impaired
 Ability to meet the ordinary demands of life is impaired

A

pyschosis

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5
Q

6 types of psycosis

A

Schizophrenia
 Bipolar Disorder with Psychotic Features
 Schizoaffective Disorder
 Major Depressive Disorder with Psychotic Features
 Psychosis due to Substance Abuse
 Psychosis due to a General Medical Condition

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6
Q

diagnosis for schizophrenia:

aracteristic Symptoms: 2 or more, each present for a significant proportion of the time for 1 month (or less if treated)

A

Delusions
 Hallucinations
 Disorganized Speech
 Grossly disorganized or catatonic behavior
 Negative symptoms (affective flattening, alogia, or avolition)

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7
Q

 Social/Occupational Dysfunction
** Signs of the disturbance present for 6
months or longer**
 Schizoaffective and mood disorders have been ruled out
 Substance abuse and general medical conditions have been ruled out
 In presence of autism, hallucinations or delusions present for over 1 month

A

what is: Diagnostic Criteria for 10 Schizophrenia

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8
Q

4 positive symptoms of schizophrenia:

A

Positive Symptoms  Delusions
 Hallucinations
 Disorganized speech
 Disorganized or catatonic behavior

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9
Q

what are the negative symptoms for schizophrenia?

4

A

Negative Symptoms
 Impoverished thoughts  Deficits of attention
 Blunt affect
 Lack of initiative

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10
Q

dopamine hypothesis

A

Investigators noted that dopamine receptor antagonists inhibited amphetamine-induced activation and stereotypical behaviors of rodents. This effect has been found to be a reasonably reliable predictor of antipsychotic activity in humans.

Other evidence supporting a role of dopamine in psychosis comes from the observation that all drugs—at least to date—capable of reducing psychosis are also dopamine receptor antagonists.

Moreover, agents associated with increased dopamine activity such as amphetamines, methylphenidate (Ritalin), or cocaine tend to cause psychosis or make it more severe.

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11
Q

receptors associated with schizophrenia

A

D2: Relieve positive symptoms
5-HT2: Relieve negative symptoms
alpha1: autonomic side effects (orthostatic hypotension, tachycardia)
H1: sedation
M: confusion, memory impairment, psychotic reactions, Provide protection against EPS

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12
Q

5 characteristics of TYPICAL antipsychotics

A

   

  1. Dopamine D2 blockers

2.Produce extrapyramidal symptoms+ (EPS) Elevate prolactin (PRL) levels

  1. Equally effective but differ in potency/side effects
  • *4.Largely effective for positive symptoms**
    (e. g., delusions, hallucinations, disorganization of thought and behavior)
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13
Q

what are three characteristics of atypical antipsychotics:

  1. which receptors ?
  2. what does addition of 5HT2A blockade add? (thinking of 2 symptoms here)
A

 Share D2 and 5HT2A antagonism in common
 Addition of 5HT2A blockade may:
 reduce EPS
 improve efficacy for negative symptoms
e.g., withdrawal, flat affect, paucity of thought, avolition (poor initiation of goal directed behavior)

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14
Q

 Phenothiazines and Thioxanthenes
 Aliphatic side chain
 Chlropromazine(Thorazine) 

which potency?

A

low

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15
Q

Piperidine ring in side chain  Thiothixene(Navane)

which desirable effect of thiothixene?

A

 LowerincidenceofEPS

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16
Q

Piperazine group in side chain
 Fluphenazine(Prolixin),Perphenazine(Trilafon) 

how strong?

A

Piperazine group in side chain
 Fluphenazine(Prolixin),Perphenazine(Trilafon)  Potent

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17
Q

which potency:

 Butyrophenones
 Haloperidol (Haldol)

A

 Butyrophenones
 Haloperidol (Haldol)  High potency

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18
Q

low potency antipsychotic that starts with a C?

A

Clozapine (Clozaril)

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19
Q

which antipsychotic?

 5-HT2/D2 antagonist
 Limited EPS at low doses
 Only approved agent for use in children and teens

A

Risperidone (Risperdal)

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20
Q

t/f. papileridone has an active metabolite

A

true

 Paliperidone (Invega) • Active metabolite

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21
Q

which atypical?

 D2 partial agonist
 Reducesactionsoffullagonist
 5-HT2A antagonist, 5-HT1A partial agonist  Lower incidence of side effects

A

Aripiprazole (Abilify)  D2 partial agonist
 Reducesactionsoffullagonist
 5-HT2A antagonist, 5-HT1A partial agonist  Lower incidence of side effects

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22
Q

which antipsychotic?
 5-HT2A, 5-HT1A, 5-HT2C/D2 antagonist  Limited EPS

A

 Ziprasidone (Geodon)
 5-HT2A, 5-HT1A, 5-HT2C/D2 antagonist  Limited EPS

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23
Q

which syndrome described?

Suppression of spontaneous movements and
complex behaviors
 Reduced initiative and interest in environment
 Decreased manifestations of emotion or affect
 Psychotic symptoms disappear over time

A

Neuroleptic Syndrome

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24
Q

Cerebral Cortex
 Minimal adaptive changes in dopamine
system

what do antipscyhotics do to seizure thresholds? which two phenothiazines most likely

A

Can lower seizure thresholds
 More likely with low potency phenothiazines(chlorpromazine, fluphenazine, perpehnazine)  Butyrophenones unpredictable
 More likely in predisposed patients

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25
Q

Basal gangial effects

Suggested that decreased dopamine activity
associated with extrapyramidal side effects (EPS)
 Antipsychotics consistently _______ dopamine metabolism
 Antipsychotic effects not thought to occur here
 Initially increase dopamine metabolism, synthesis and firing rate
 Diminisheswithtime

A

increase

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26
Q

CNS effects:

limbic system:

Limbic System
 Thought to be site of __________ effects
 Anticholinergics do not block therapeutic effect

note: Anticholinergics do not affect DA turnover in limbic system

A

antipsychotic effects

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27
Q

CNS effects hypothalamus:

which three effects?

which patients do you avoid in?

A

 Increased prolactin secretion  Little tolerance
 Avoid in patients with established breast carcinoma

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28
Q

which two antipsychotics increase prolactin the most?

A

reisperidone and palperidone

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29
Q

3 antipsychotics with moderate increase in prolactin

close

old

Z

A

clozapine

olanzapine

ziprasidone

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30
Q

quetiapine and aripirazole dopamine increase?

A

no increase

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31
Q

4 Clinical Consequences of Sustained Hyperprolactinemia

A

Sexual dysfunction
! Amenorrhea
! Gynecomastia/Galactorrhea
! Hypoestrogenism/Osteopenia?

32
Q

brain stem effects?

A

Brainstem
 Little effect on respiration
 Decreased vasomotor reflexes
 Occurs at low doses

33
Q

chemoreceptor trigger zone effects?

A

Chemoreceptor Trigger Zone
 Protect against nausea and vomiting elicited by activation of dopamine receptors
 Occurs at low doses

34
Q

which drug may act as diuretic?

A

Renal System
 Chlorpromazine may be antidiuretic

35
Q

Endocrine System

 Impairs glucose tolerance  Decreases insulin release

which drug?

A

Endocrine System
** Chlorpromazine**
 Impairs glucose tolerance  Decreases insulin release

36
Q

which drugs increase the risk of type II diabetes?

A

Clozapine, risperidone, aripiprizole, ziprasidone, olanzepine and quetiapine

37
Q

Mild orthostatic hypotension
 More so with ______and ________
 Less so with which 3 drugs?  Tolerance develops

A

Mild orthostatic hypotension
 More so with chlorpromazine, thioridazine
 Less so with haloperidol, loxapine, risperidone  Tolerance develops

38
Q

___________relationship between antimuscarinic potency and EPS

A

inverse

39
Q

t/f. antipsychotics may May increase acetylcholine turnover

 Mainly basal ganglia

A

true

40
Q

what type of ADE below:

Nasal stuffiness
 Dry mouth
 Blurred vision
 Constipation
 Cardiovascular
 Orthostatic Hypotension

A

anticholinergic

41
Q

name the 6 extrapyramidal symptoms of antipsychotics?

AD PP Tardive syndrome

Prominent during treatment with high potency neuroleptics.
Less likely with clozapine, thioridazine or low dose risperidone.
First 4 side effects occur early on. Last 2 are delayed in onset.

A

 Acute Dystonia
 Akathesia
 Parkinsonian Syndrome
 Neuroleptic Malignant Syndrome  Perioral Tremor
 Tardive Dyskinesia

42
Q

what are the symptoms of acute dystonia?

how do you treat it?

A

Symptoms
 Muscle spasms
 Facial Grimacing
 Torticollis: stiff neck and Oculogyeric crisis

Treatment
 Anticholinergic antiparkinsonian agents

43
Q

what are the symptoms of Parkinsonian syndrome: (recall TRAP)

how do you tx parkinsonian syndrome? (2 ways here)

A

** Symptoms:** Akinesia, Mask facies, Decreased arm movement, Rigidity, Tremor

 Treatment
 Anticholinergic antiparkinsonian agents  Amantadine

44
Q

why should you not treat parkinsonian syndrome with Bromocriptine or levo-dopa?

A

Maybe indistinguishable from idiopathic PD. Develops gradually. Levodopa or bromocriptine will induce agitation and enhance psychosis. First 5-30 days.

45
Q

which syndrome?

 Rare
 Fever
 Severe Parkinsonism with catatonia
 Fluctuations in coarse tremor intensity  Autonomic instability
 Elevated creatine kinase
 Myoglobinemia
 High mortality (10%)

A

neuroleptic malingnant syndrome

46
Q

how do you tx neuroleptic malignant syndrome?

3 ways

A

Treatment
 Immediate cessation of antipsychotic  Supportive care
 Dantrolene or bromocriptine may help

47
Q

what is perioral tremor? how comon? how do you tx/

A

Rare
 Rabbit syndrome
 Treat with anticholinergic agents  Stop neuroleptic

48
Q

what is described here:

Stereotyped, repetitive, quick choeriform (tic-like) movements of face eyelids (blinks or spasms), mouth (grimaces), tongue, extremities or trunk
 No adequate treatment
 Discontinue antipsychotic
 Symptoms fade with time

A

Tardive Dyskinesia

49
Q

 5% of patients on chlorpromazine
 More common with phenothiazines  Occur in first 8 weeks
 Skin clears with discontinuation

which reaction?

A

urticaria or dermatitis

note photosensivity as well

50
Q

which drugs most likely to cause weight gain?

A

clozapine and olanzapine

51
Q

moderate risk of weight gain?

quiet risper

A

 Risperidone, Quetiapine, intermediate risk

52
Q

less likely to cause weight gain?

A

Ziprasidone, Aripiprazole, Asenapine less likely

53
Q

which syndrome described below:

 Abdominal obesity
 Atherogenic dyslipidemia (blood fat disorders — high triglycerides, low HDL cholesterol and high LDL cholesterol)
 Elevated blood pressure
 Insulin resistance or glucose intolerance
 Prothrombotic state (e.g., high fibrinogen or
plasminogen activator inhibitor–1)
 Proinflammatory state (e.g., elevated C-reactive protein)

A

metabolic syndrome

54
Q

which drug most likley to cause metabolic syndrome?

A

olanzapine

55
Q

which two drugs moderate risk of metabolic syndrome?

quiet risper

A

quetiapine

risperidone

56
Q

which two drugs low risk of metabolic syndrome?

A

ziprasidone

aripiprazole

57
Q

mech of ADE:

EPS & hyperprolactinemia—
 Hypotension—
 Sedation—
 Weight gain—
 Anticholinergic (e.g., dry mouth)—
 Sexual side effects—

note

A

EPS & hyperprolactinemia—D2 blockade
 Hypotension—alpha adrenergic blockade
 Sedation—histaminergic blockade
 Weight gain—histaminic & serotonergic blockade
 Anticholinergic (e.g., dry mouth)—muscarinic blockade
 Sexual side effects—serotonergic, muscarinic, noradrenergic and D2 (via prolactin) blockade

Note:

58
Q

t/f. Typical antipsychotics may produce extrapyramidal side effects compared to atypical which are unlikely to. Potent antipsychotics have increased risk of EPS while weak agents have additional sedative, hypotensivie and autonomic side effect.

A

true

59
Q

pharmacokinetics of anti-psychotics:

when is bioavailabilityincrease?

are they lipophilic?

protein bound?

where do they accumulate?

can they cross placental barrier?

A

ral absorption erratic
 Bioavailability increase 4-10x when given
intramuscularly
 Highly lipophilic
 Highly protein and membrane bound
 Accumulates in high blood supply tissues
 Crosses placental barrier and enters breast milk

60
Q

more pharmkinetics 

Peak plasma concentration attained 2-4 hr after administration
 Disappearance from plasma includes:  Rapid redistribution phase t1/2= 2hr
 Slow early elimination t1/2= 30 hr
** Elimination t1/2= 20-40 hr**
 Biological effect usually lasts 24 hr  Give entire daily dose at once

A
61
Q

what is main route of metabolism?

what are exceptions to this?

A

Oxidation main route
 Hepatic microsomal oxidases and conjugation

Exceptions
7-OH-chlorpromazine
 Several N-methylated metabolites of phenothiazines  Paliperidone (Inega)
 Dehydroaripirazole

62
Q

describe tolerance/physical dependance of these drugs?

A

Not addicting
 Some physical dependence
 Malaise, difficulty sleeping if abrupt stoppage
 Tolerance develops to sedative effects over days to weeks

63
Q

important to note:

 Typical Antipsychotics
 Metabolized at 2D6 and 3A4
 Do not induce P 450 enzymes
 Many inhibit 2D6
 Raise levels of many TCAs and SSRIs
 Raise levels of many other antipsychotics
 Theoretically vulnerable to inducers and inhibitors of 2D6 and 3A4, though little is known about this in vivo

A
64
Q

tx of psychsis

 Useful for most psychoses  Target symptoms
 Tension, hyperactivity, combativeness, hostility, hallucinations, acute delusions, insomnia, anorexia, poor self care, negativism, withdrawal

A
65
Q

how do you tx schizophrenia?

A

 Schizophrenia  Antipsychotics

66
Q

how do you tx bipolar disorder?

A

Bipolar Disorder with Psychotic Features  Mood stabilizers and/or antipsychotics

67
Q

how do you tx schizoaffective disorder?

A

 Schizoaffective Disorder
 Antipsychotics, with mood stabilizers and/or
antidepressants

68
Q

how do you tx:

Major Depressive Disorder with Psychotic Features

A

ECT and/or antidepressant medication and/or antipsychotic medication

69
Q

how do you tx: Psychosis due to Substance Abuse intoxication/withdrawal

A

 Definitive treatment of substance abuse condition
 Antipsychotics as an adjunct for delirium

70
Q

how do you tx psychosis due to a gernelar medical condition?

A

 Definitive treatment of general medical condition with antipsychotics as an adjunct

71
Q

Trial and error
 Choice based on side effects
 If patient responded well to a drug in the past, use again

A
72
Q

Long acting depot antipsychotics

! Can be administered in such a way that after a single dose a therapeutically efficient tissue concentration of a least one week

A

know

73
Q

be aware:

Three depot preparations are currently available ! Prolixin Decanoate
! Haldol Decanoate
! Risperidal Consta

A
74
Q

when should depot preps be considered?

Depot preparations should be considered:

A

For patients with several relapses who
consistently default on oral medications

 In those patients who have clear cut compliance
problems

 When oral absorption is poor due to idiosyncratic
pharmacokinetic reactions

75
Q

4 misc use of anti-psychotics?

A

 Nausea and vomiting
 Alcoholic hallucinosis
Neuropsychiatric diseases marked by movement disorders
 Tourette

76
Q

 Strong subjective feelings of distress or
discomfort often referred to the legs

A

akathesia

Psychiatry (11 decks)

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