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ICOM - Mental Health > Belovich- Antipsychotics/ Atypicals > Flashcards

Belovich- Antipsychotics/ Atypicals Flashcards

1
Q

FGAs/SGAs have improved efficacy against positive symptoms

A

SGAs

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2
Q

Atypicals/ typicals have a reduced risk for EPS, due to less potency for D2 receptors

A

typicals

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3
Q

Atypical antipsychotics are associated with a syndrome that may increase the risk of coronary artery disease, stroke, and hypertension

A

metabolic

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4
Q

Clinical effects of atypicals is due to which 2 MOAs?

A

D2R antagonism and inverse agonism of 5-HT2A

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5
Q

Agonism of 5-HT2A and 5-HT2C receptors is basis for activity of these lsd and mescaline

A

hallucinatory

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6
Q

Hallucinatory properties of LSD and mescaline led to investigation ofas a basis for schizophrenic symptoms

A

serotonin

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7
Q

Agonism of 5-HT2A receptors leads to depolarization of neurons, which stabilizes NMDA receptors

• Increased activity may increase psychotic symptoms

A

glutamatergic

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8
Q

Agonism of 5-HT2C receptors (increased seratonin signaling) inhibits cortical and limbic release

A

dopaminergic

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9
Q

What type of agonist:

  • elicits maximum biological response
A

full agonist

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10
Q

What type of agonist:

prevents agonist from binding, but does not effect basal activity

A

antagonist

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11
Q

What type of agonist?

elicits partial maximum response

always antagonist to full agonist

A

partial agonist

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12
Q

What type of agonist?

prevents agonist from binding, and stabilizes inactive form

desreased in baseline activity

freezes receptor

can be synonymous with antagonist

A

inverse agonist

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13
Q

Atypical antipsychotic agents have less effect on , but more effect on receptors than typical antipsychotic agents

A

D2Rs

5-HT2A

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14
Q

Agonism of 5-HT2A receptors leads to depolarization of neurons, stabilizes NMDA receptors

• Inverse agonism increases/reduces activity of these neurons

A

glutamatergic

reduces

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15
Q

Agonism of 5-HT2C receptors cortical and limbic dopaminergic release

• Inverse agonism of and 5-HT2C receptors may therefore lead to increased/decreased DA in mesocortical structures, but D2 antagonistic properties balance this

A

increased

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16
Q

ADRs of Antipsychotic agents share close relationship with D2R

A

affinity

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17
Q

Atypical antipsychotics have lower D2R potency which results in fewer/more on-target ADRs, fewer/more off-target ADRs

A

fewer on-target

more off-target

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18
Q

Most of the drugs in which group of antipsychotics often produce substantial weight gain?

A

atypicals

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19
Q

Atypicals have an Increased risk of development of diabetes mellitus, which 2 in particular?

A

olanzapine

clozapine

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20
Q

Though it is recommended to monitor patients taking atypicals due to ADRs, whcih one in particular is it required to monitor?

Personal and family history of obesity, diabetes, dyslipidemia, hypertension, and cardiovascular disease • Weight and height (so that body mass index can be calculated) • Waist circumference (at the level of the umbilicus) • Blood pressure • Fasting plasma glucose level • Fasting lipid profile

A

clozapine

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21
Q

While taking atypicals, Regular monitoring of patients with preexisting diabetes should include and sometimes insulin

A

hemoglobin A1C (HgA1C)

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22
Q

What group of antipsychotics is the first line for treatment of schizophrenia?

A

atypicals (except clozapine due to risk of agranulocytosis or bowel obstruction)

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23
Q

Why is clozapine the only atypical not suggested for first line treatment?

A

risk of agranulocytosis (decreased neutrophils) and bowel impaction

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24
Q

What is the concern with elderly patients with dementia-related psychoses and taking atypcials?

A

increased risk of stroke

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25
Q

Which type of drugs can treat all of the following conditions?

  • Schizophrenia (first line, except clozapine)
  • Acute mania
  • Adjunctive therapy in treatment-resistant depression
  • Adjunctive therapy in major depressive disorder
  • Post-traumatic stress disorder
  • Anxiety disorders
  • Behavioral disturbances associated with dementia

Also effective for treating psychotic depression and for psychosis secondary to head trauma, dementia, or treatment drugs

A

atypicals

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26
Q

Other than primary psychosis, atypicals can be used to treat psychotic depression and for psychosis secondary to head trauma, , or treatment drugs

A

dementia

27
Q

Which atypical is reserved for individuals who are refractory to all other antipsychotic agents

• Not a first-line agent because of hematological side effects (hematological)?

A

clozapine

28
Q

What atypical can be used as a treatment with persons with severe tardive dyskinesia?

A

clozapine

29
Q

Which atypical is a good treatment of persons with a low threshold for EPS?

A

clozapine

30
Q

Which atypical is Highly effective in treating mania and depression though carries a strong risk of hematological side effects?

A

clozapine

31
Q

What is the MOA of clozapine?

A

Atypical, inverse agonist of 5-HT2a and low affinity D2 receptor antagonist

32
Q

What is the most stereotypical ADR for atypicals?

A

sedation

33
Q

What are some common minor ADRs of clozapine and what are some more severe ADRs that affect cardiovascular and hematological systems?

A

minor- sedation, weight gain, constipation

major cardiovascular- myocarditis, cardiomyopathy

major hematological- leukopenia, granulocytopenia, agranulocytosis

34
Q

Clozapine should be discontinued if the WBC count is below cells/mm3 or the granulocyte count is below 1,500 cells/mm3

A

3,000

35
Q

Why must the patient’s baseline of WBCs be monitored while taking clozapine?

A

Due to possiblility of decrease neutrophile numbers

36
Q
  • white blood cell (WBC) count below 3,500 cells/mm3
  • previous bone marrow disorder
  • history of agranulocytosis during clozapine treatment

are contraindications for which atypical?

A

clozapine

37
Q
  • Schizophrenia
  • Bipolar Disorder
  • Autism Spectrum Disorder
  • Adjunctive treatment in major depressive disorder

are all indications for the atypical drug?

A

aripiprazole

38
Q

What is the MOA of aripiprazole?

A

Aripiprazole is a partial agonist of D2 and 5-HT1A

and an antagonist or inverse agonist of 5-HT2a

39
Q

Which atypical is more friendly for on and off target ADRs?

A

aripiprazole

40
Q

Which atypical treats the following indications?

  • Schizophrenia
  • Acute treatment of manic or mixed episodes with bipolar I
  • Maintenance treatment of bipolar I
  • Treatment-resistant depression with fluoxetine
A

olanzapine

41
Q

What is the MOA of olanzapine?

A

antagonist of 5-HT2a, D2, muscarinic, and H1 receptors

42
Q

Other than typical side effets of atypicals, which atypical as ADRs for :

Somnolence, dry mouth, dizziness, constipation, dyspepsia, increased appetite

  • Dose-related risk of EPS (akathesia, tremor)
  • Transaminase elevation
A

olanzapine

43
Q

What is a major black box warning for olanzapine?

A

Cardiorespiratory arrest and sudden death

44
Q

Which atypical is used for the following indications?

  • Schizophrenia
  • Acute treatment of manic episodes with bipolar I
  • Bipolar depression
  • Off-label uses for sleep, anxiety, delirium at low doses
A

quetiapine

45
Q

What is the MOA of quetiapine?

A

weak antagonist of D2 and 5HT2

46
Q

Which atypical is the Least likely to cause EPS (with the exception of primavanserin), regardless of dose?

A

Quetiapine

47
Q

What is the medication most Preferred in Patients with Parkinson disease who develop dopamine agonist–induced psychosis?

A

Quetiapine due to being the least likely to cause EPS

48
Q

Though quetiapine is the least likely to cause EPS (with exception of primavanserin) , there are DDI’s with drugs that increase what cardiovascular effect?

A

DDI’s with drugs that increase QTc interval

49
Q

Which antipsychotic is best for the follwing indications:

  • Acute and maintenance treatment of schizophrenia in adults and adolescents age 13 - 17 years
  • Acute manic episodes in bipolar I disorder (ages 10+)
  • Irritability associated with ASD in ages 5 - 16 years
A

risperiodone

50
Q

What is the MOA of risperidone?

A

Antagonist of 5-HT2A, D2, 𝛼-adrenergic (low affinity), and H1 receptors

51
Q

What are the 2 drugs of choice for first-break psychosis in a young person?

A

risperidone and aripiprazole

52
Q

Which atypical elevates prolactin secretion?

A

risperidone

53
Q

Rate of relapse (psychosis) may be lower with atypical/typical antipsychotic agents

A

atypical

54
Q

Two or more psychotic episodes secondary to schizophrenia usually require years treatment

A

5

55
Q

How are most antipsychotics metabolized?

A

First-pass metabolism

56
Q

Few/Most antipsychotic drugs are highly lipid soluble and protein bound (92–99%)

A

Most

57
Q

At clinical doses, antipsychotic drugs do/do not usually interfere with the metabolism of other drugs

A

do not

58
Q

More Pharmacodynamic/Pharmakokinetic DDI’s are more commonly observed

A

Pharmacodynamic DDI’s

59
Q

• The low end of the dosage range in should be tried for at least weeks

A

several

60
Q

What are the 4 concerning types of drugs that should be avoided due to pharmacodynamics additive effects?

A

Sedatives

  • α-adrenoceptor blockers (hypotension)
  • anticholinergic drugs
  • quinidine-like action (thioridazine and ziprasidone, an atypical) due to hypotension
61
Q

Overdose antipsychotic agents are rarely fatal, with the exception of

A

thioridazine

62
Q

What do the following symptoms indicate in someone taking antipsychotics?

A

coma, convulsion, miotic pupils, deep tendon reflexes decreased

hypotension, hypothermia, ventricular tachyarrrhthmias (thioridazine)

63
Q

Management of overdoses of thioridazine is complicated by cardiac arrhythmias, is similar to that for antidepressants

A

tricyclic

64
Q
A

ICOM - Mental Health (24 decks)

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