Belovich- Antipsychotics/ Atypicals

Question 1

FGAs/SGAs have improved efficacy against positive symptoms

Answer 1

SGAs

Question 2

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

Answer 2

typicals

Question 3

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

Answer 3

metabolic

Question 4

Clinical effects of atypicals is due to which 2 MOAs?

Answer 4

D2R antagonism and inverse agonism of 5-HT2A

Question 5

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

Answer 5

hallucinatory

Question 6

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

Answer 6

serotonin

Question 7

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

• Increased activity may increase psychotic symptoms

Answer 7

glutamatergic

Question 8

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

Answer 8

dopaminergic

Question 9

What type of agonist:

• elicits maximum biological response

Answer 9

full agonist

Question 10

What type of agonist:

prevents agonist from binding, but does not effect basal activity

Answer 10

antagonist

Question 11

What type of agonist?

elicits partial maximum response

always antagonist to full agonist

Answer 11

partial agonist

Question 12

What type of agonist?

prevents agonist from binding, and stabilizes inactive form

desreased in baseline activity

freezes receptor

can be synonymous with antagonist

Answer 12

inverse agonist

Question 13

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

Answer 13

D2Rs

5-HT2A

Question 14

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

• Inverse agonism increases/reduces activity of these neurons

Answer 14

glutamatergic

reduces

Question 15

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

Answer 15

increased

Question 16

ADRs of Antipsychotic agents share close relationship with D2R

Answer 16

affinity

Question 17

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

Answer 17

fewer on-target

more off-target

Question 18

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

Answer 18

atypicals

Question 19

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

Answer 19

olanzapine

clozapine

Question 20

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

Answer 20

clozapine

Question 21

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

Answer 21

hemoglobin A1C (HgA1C)

Question 22

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

Answer 22

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

Question 23

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

Answer 23

risk of agranulocytosis (decreased neutrophils) and bowel impaction

Question 24

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

Answer 24

increased risk of stroke

Question 25

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**

Answer 25

atypicals

Question 26

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

Answer 26

dementia

Question 27

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)?

Answer 27

clozapine

Question 28

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

Answer 28

clozapine

Question 29

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

Answer 29

clozapine

Question 30

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

Answer 30

clozapine

Question 31

What is the MOA of clozapine?

Answer 31

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

Question 32

What is the most stereotypical ADR for atypicals?

Answer 32

sedation

Question 33

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

Answer 33

minor- sedation, weight gain, constipation major cardiovascular- myocarditis, cardiomyopathy major hematological- leukopenia, granulocytopenia, agranulocytosis

Question 34

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

Answer 34

3,000

Question 35

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

Answer 35

Due to possiblility of decrease neutrophile numbers

Question 36

* 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?

Answer 36

clozapine

Question 37

* Schizophrenia * Bipolar Disorder * Autism Spectrum Disorder * Adjunctive treatment in major depressive disorder are all indications for the atypical drug?

Answer 37

aripiprazole

Question 38

What is the MOA of aripiprazole?

Answer 38

Aripiprazole is a **partial agonist** of D2 and 5-HT1A and an antagonist or inverse agonist of 5-HT2a

Question 39

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

Answer 39

aripiprazole

Question 40

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

Answer 40

olanzapine

Question 41

What is the MOA of olanzapine?

Answer 41

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

Question 42

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

Answer 42

olanzapine

Question 43

What is a major black box warning for olanzapine?

Answer 43

Cardiorespiratory arrest and sudden death

Question 44

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**

Answer 44

quetiapine

Question 45

What is the MOA of quetiapine?

Answer 45

**weak** antagonist of D2 and 5HT2

Question 46

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

Answer 46

Quetiapine

Question 47

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

Answer 47

Quetiapine due to being the least likely to cause EPS

Question 48

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

Answer 48

DDI’s with drugs that increase QTc interval

Question 49

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

Answer 49

risperiodone

Question 50

What is the MOA of risperidone?

Answer 50

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

Question 51

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

Answer 51

risperidone and aripiprazole

Question 52

Which atypical elevates prolactin secretion?

Answer 52

risperidone

Question 53

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

Answer 53

atypical

Question 54

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

Answer 54

5

Question 55

How are most antipsychotics metabolized?

Answer 55

First-pass metabolism

Question 56

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

Answer 56

Most

Question 57

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

Answer 57

do not

Question 58

More **Pharmacodynamic/Pharmakokinetic** DDI’s are more commonly observed

Answer 58

Pharmacodynamic DDI's

Question 59

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

Answer 59

several

Question 60

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

Answer 60

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

Question 61

Overdose antipsychotic agents are rarely fatal, with the exception of

Answer 61

thioridazine

Question 62

What do the following symptoms indicate in someone taking antipsychotics?

Answer 62

coma, convulsion, miotic pupils, deep tendon reflexes decreased hypotension, hypothermia, ventricular tachyarrrhthmias (thioridazine)

Question 63

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

Answer 63

tricyclic