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ICOM - Mental Health > Belovich- Antipsychotic medications I > Flashcards

Belovich- Antipsychotic medications I Flashcards

1
Q

Main 5 indications for antipsychotics?

A
  • Schizophrenia*- most common
  • Bipolar disorder (plus mood stabilizing effect)
  • Psychotic depression
  • Dementia-related psychoses
  • Drug-induced psychoses
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2
Q

Though not drug of choice for nonpsychotic patients, Can treat anxiety symptoms in

A

autism spectrum disorder (risperidone)

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3
Q

Antipsychotics can improve mood, reduce anxiety, and reduce disturbances

A

sleep

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4
Q

some antipsychotics can be used as antiemetics due to antagonism of receptors in the area postrema

A

dopamine

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5
Q

What are the 3 antipsychotics used for their antiemetic effects?

A
  • Ondansetron (Zofran)
  • Scopolamine (Transderm Scop)
  • Dimenhydrinate (Dramamine)
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6
Q

Histamine receptor antagonism can treat which itchy disease?

A

Pruritis

(nerve itcthing)

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7
Q

What are the indications for antipsychotic agents that do not tx some kind of psychosis?

A

antiemetics

pruritis

preoperative sedatives

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8
Q

What causes the positive symptoms (hallucinations, delusions) are caused by Hyperactivity of DA in pathway

A

mesolimbic

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9
Q

D2R helps alleviate psychotic symptoms

A

antagonism

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10
Q

Levodopa, amphetamines, bromocriptine, apomorphine, etc. can schizophrenia psychosis or produce psychosis de novo in some patients. Why?

A

aggravate; due to increased activity of dopamine receptors

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11
Q

What is the assumed cause of Negative symptoms (emotional blunting, social withdrawal, lack of motivation) and cognitive impairment of schizophrenia?

A

DA-receptor hypofunction in the prefrontal cortex

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12
Q

Presynaptic D1 receptors in the prefrontal cortex thought to modulate activity, which, if impaired, can decrease the activity leading to impaired cognition and working memory.

A

glutamatergic

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13
Q

Currently, negative symptoms can/cannot be pharmacologically targeted

A

cannot

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14
Q

Which neurotransmitter pathway is affected when a D2R blockade results in:

Alleviates psychotic symptoms

• May induce other behavioral symptoms

A

mesocorticomesolimbic pathway

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15
Q

What happens with D2R blockade in nigrostriatal pathway?

A

Produces motor disturbances by two opposing mechanisms (Extrapyramidal Symptoms and Tardive Dyskinesia)

-imbalance of AcH and DA levels

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16
Q

Increases prolactin secretion

• Likely responsible for altered metabolism

occur when the D2R is blocked in which dopamine pathway?

A

D2R blockade tuberoinfundibular pathway

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17
Q

What causes Parkinsonism like symptoms because of excess acetylcholine signaling relative to dopamine signaling and what dopamine pathway is effected?

A

The used of antipsychotics that block D2R in the nigrostriatal pathway

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18
Q

Hyperprolactinemia, caused by D2R blockade in tuberoinfundibular pathway, can lead to which side effects?

A

increased breast tissue

lactation

gynecomastia

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19
Q

Antipsychotic drugs have similar/various efficacy

A

similar

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20
Q

Most important factor of successfor schizophrenia is spent on a drug

A

time

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21
Q

Combination therapy should only be used in patients

A

refractory

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22
Q

The main clinical effects of FGA typical antipsychotics is antagonism

A

D2R

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23
Q

Potency of typical antipsychotics is with ADRs

A

correlated

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24
Q

Atypical (or “second generation”) antipsychotics clincal effects are due to which 2 MOAs?

A

D2R antagonism and inverse agonism of 5-HT2A

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25
Q

Why are atypical antipsychotics more commonly presribed?

A

more efficacious and friendlier ADRs

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26
Q

What are the 3 main classes of typical antipsychotics?

A

Phenothiazines

• Chlorpromazine • Fluphenazine

• Thioxanthenes

• Thiothixene

• Butyrophenones

• Haloperidol

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27
Q

What are the 2 antipsychotics in the phenothiazine class (FGA)?

A
  • Chlorpromazine
  • Fluphenazine
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28
Q

What is the FGA antipsychotic in the thioxanthenes class?

A

thiothixene

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29
Q

What is the FGA antipsychotic in the butyrophenones class?

A

haloperidol

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30
Q

ANS ADRs due to antipsychotics depends on the .

A

potency

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31
Q

Neurologic effects, Neuroleptic Malignant Syndrome, and Behavioral Effects

are more commone typicals/atypicals?

A

typical antipsychotics

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32
Q

Metabolic ADRs are more common in typical/atypical agents

A

atypical

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33
Q

hyperprolactinemia is more common in atypical/typical agents

A

typical

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34
Q

Which antipsychotic is more likely to cause toxic or allergic reactions?

A

clozapine

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35
Q

Cardiac toxicity ADRs can occur with atypicals/typicals/both?

A

both

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36
Q
A
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37
Q

Typical antipsychotics can also act as antagonists for which 3 other receptor types (off target) other than dopamine receptors?

A

• 𝛼-adrenergic antagonists - orthostatic hypotension, light-headedness

• Muscarinic antagonists - anticholinergic effects, dry mouth, urinary retention

• H1 antagonists - sedation, weight gain

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38
Q

The following off target effects of typical antipsychotics is due to antagonism of

receptors?

orthostatic hypotension, light-headedness

A

a-adregergic

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39
Q

The following off target effects of typical antipsychotics is due to antagonism of

receptors?

anticholinergic effects, dry mouth, urinary retention

A

Muscarinic

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40
Q

The following off target effects of typical antipsychotics is due to antagonism of

receptors?

sedation, weight gain

A

H1

41
Q

ADRs of Antipsychotic agents share close relationship with D2R

A

affinity

42
Q

Potency governs ADR profiles of antipsychotics and severity more than

A

efficacy

43
Q

more potent= higher

A

affinity

44
Q

Typicals have a higher/lower affinity for D2 receptors

A

higher

45
Q

In general, higher potency agents are given at doses, while lower potency agents may dosed

A

lower; higher

46
Q

More potent antipsychotics will have less/more occurrence of off target ADRs?

A

less

47
Q

More potent antipsychotics wil have strong on target ADRs such as :

A

EPS and TD

48
Q

Blockade of D2 receptors alters balance

A

DA/ACh

49
Q

Relative excess cholinergic influence results in EPS/TD?

A

EPS (excess Ach as compared to DA)

50
Q

What are the EPS ADRs?

A

Dystonias (sustained contraction of muscles leading to twisting, distorted postures)

  • Parkinson-like symptoms
  • Akathisia (motor restlessness)
51
Q

EPS/TD symptoms are generally reversible?

A

EPS

52
Q

Drugs that have stronger/weaker anticholinergic activity have a lower risk of developing EPS

A

stronger as the imbalance of Ach to DA is less

53
Q

“Neuroleptic” refers to potency typical antipsychotic drugs

• High incidence of extrapyramidal side effects at clinically effective doses

A

high

54
Q

What type of drugs are effective at treating extrapyramidal symptoms acute dystonia and Parkinsonism?

A

Antiparkinsonian agents

• Amantadine, a prodopaminergic drug, increases effective dopamine signaling

• Benztropine, an anticholinergic drug, can counter the effects of “excess” cholinergic effects

• Antimuscarinic effects can occur

55
Q

Which type of antiparkonsonian agent that is used to combat extrapyramidal symptoms caused by typical antipsychotics should not be used with an Alzheimer’s co-morbidity?

A

Benztropine, an anticholinergic drug, can counter the effects of “excess” cholinergic effects

56
Q

Which Antiparkinsonian agents, effective for acute dystonia and Parkinsonism due to EPS from typical antipsychotics, is a prodopaminergic drug, increases effective dopamine signaling and restores the Ach/DA imbalance?

A

Amantadine

57
Q

Which Antiparkinsonian agents is an anticholinergic drug and can counter the effects of “excess” cholinergic activity due to typical antipsychotics?

A

Benztropine

58
Q

What non Antiparkinsonian agents is also effective for acute EPS?

A

Diphenhydramine

59
Q

Akathesia (restlessness), an EPS symptom, a is more effectively managed with (benzodiazepines) or (ßblockers)

A

clonazepam

propranolol

60
Q

EPS/TD symptoms are generally irreversible?

A

TD

61
Q

Excess and Involuntary movements, bilateral and facial jaw movements, “fly-catching” or “worm-like” tongue movement

A

Tardive dyskinesia (TD)

62
Q

TD occurs with short/long-term treatment with antipsychotic agents

A

long-term

63
Q

Which ADR occurs when Dopaminergic receptors become sensitized due to chronic antagonism?

Also, Neuronal response to dopaminergic input overpowers response to cholinergic input cause the symptoms?

A

TD

64
Q

Describe the Ach/DA imbalance that caused TD symptoms?

A

excess dopamine activity compared to Ach activity from sensitization of dopamine receptors

65
Q

TD is more commonly observed with high/low potency agents (esp. haloperidol)

A

high

66
Q

What are the 2 types of treatments for Tardive dyskinesia?

A

• Drug cessation • Symptoms may improve but in many cases TD is irreversible and persistent

• VMAT inhibitors • Reduce amount of DA available to release • (valbenazine and deutetrabenazine)

67
Q

What are the 2 types of vesicular monoamine transporter inhibitors that are used to combat TD?

A

valbenazine and deutetrabenazine

68
Q

What is the MOA of VMAT inhibitors?

A

Reduce amount of DA available to release because they inhib the vesicular monoamine transporter that packs the synaptic vescicles for release

69
Q

NMS occurs due to D2R blockade in the and nigrostriatal pathways

A
70
Q

NMS is an on/off target ADR?

A

on

71
Q

What condtion is being described:

  • Muscle rigidity (“lead-pipe rigidity”)
  • Fever
  • Altered mental status and stupor
  • Unstable blood pressure,
  • Myoglobinemia,
  • Elevated serum creatine kinase
  • Rare, but fatal in 10-20% of cases if untreated
A

NMS

72
Q

Most frequent with high doses of potent agents (a.k.a. “ agents”)

A

neuroleptic

73
Q

NMS is more/less common in atypical agents

A

less

74
Q

What 3 things are considered in the treatment of NMS?

A

Discontinue use of the antipsychotic agent

dantrolene*

bromocriptine*

75
Q

What 2 drugs can be used to treat NMS associated with antipsychotic agent?

A

dantrolene

bromocriptine

76
Q

How long can NMS persist after the offending agent is discontinued?

A

more than a week

77
Q

NMS symptom persistence is associated with

A

mortality

78
Q

How do we distinguish neurological ADRs (most likely caused by FGAs)?

A

distinguish by duration of symptoms

79
Q

and D2R antagonism can result in akinesia, and dysphoria

A

D1R

80
Q

“diminished spontaneity,” apathy, withdrawal, appearance of depression

A

akinesia (negative symptom)

81
Q

Delirium and psychosis can be induced by small/large doses of typical antipsychotics

A

large

82
Q

Which population can develop pseudomementia (confusion and disorientation) from taking antipsychotics?

A

elderly

83
Q

Blockade of D2Rs in pathway causes hypersecretion of prolactin by pituitary

A

tuberoinfundibular

84
Q

can directly induce galactorrhea, and sexual dysfunction or infertility in women and men

A

Hyperprolactinemia

85
Q

What is an effective method to treat hyperprolactinemia?

A

Dosage reduction/cessation (however, keep in therapeutic range)

86
Q

When switching antipsychotic agents in the case of hyperprolactinemia is not feasible, which 2 drugs can be used?

A

bromocriptine

aripiprazole

87
Q

Low-potency frequently cause orthostatic hypotension and tachycardia due to off target a-adrenergic effects

A

phenothiazines

88
Q

What are the cardiovascular effects of FGA phenothiazines due to off target blockade of adgenergic receptors?

A

Mean arterial pressure, peripheral resistance, and stroke volume are decreased

89
Q

Phenothiazine agents (low potency than other FGAs) produce more (H1) and weight gain than other typical antipsychotics due to off target effects.

A

sedation

90
Q

Low potency phenothiazines associated with increased serum and hyperglycemia.

A

triglycerides and hyperglycemia

91
Q

Chlorpromazine and are the least potent of the phenothiazine class

A

thioridazine

92
Q

Which phenothiazine is no longer used due to being associated with torsades de pointes?

A

• Thioridazine

93
Q

Which phenothiazine is high potent and has a high potential for EP but Low potential for weight gain, sedation, and orthostasis?

A

fluphenazine

94
Q

Which highly potent typical antipsychotic phenothiazine is Commonly used in long-acting injectable formulation for noncompliant patients?

A

Fluphenazine

95
Q

What is the most potent and widely used typical antipsychotic?

A

Haloperidol

96
Q

Which FGA has Greater incidence of EPS compared to other typical antipsychotics?

A

haloperidol

97
Q

Which FGA is described:

Greater incidence of EPS compared to other typical antipsychotics

  • Low potential for orthostasis, weight gain, sedation
  • Can be used to manage acute psychotic states
  • Commonly used in long-acting injectable formulation for noncompliant patients
A

haloperidol

98
Q

Which highly potent typical commonly used in long-acting injectable formulation for noncompliant patients Can be used to manage acute psychotic states?

A

haloperidol

99
Q
A

ICOM - Mental Health (24 decks)

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