Antipsychotic Drugs

Question 1

paliperidone

Answer 1

TRADE: Invega
CLASS: atypical antipsychotic
FDA approval: tx of schizophrenia & schizoaffective disorder in adults
MAIN POINTS:
1) primarily antagonizes D2 and 5HT2A (serotonin) receptors
2) its flexible route of administration options makes it useful for the management of psychotic disorders
3) it is effective, however, its side-effect profile may vary in tolerability

Question 2

xanomeline-trospium

Answer 2

TRADE: KarXT
CLASS: muscarinic antagonist (type of anticholinergic agent)
FDA approval: no, but maybe later this yr
MAIN points:
1) two separate drugs used together, the first of which is used to help treat positive and negative symptoms of schizophrenia and Alzheimer’s. the second of which helps prevent the side effects the first can cause
2) more recent drug, few studies, small population of people who have consumed the drug
3) novel mechanisms –> no dopamine affinity; improves cognition AND reduces psychosis

Question 3

lumaterperone

Answer 3

TRADE: Caplypta
CLASS: second-generation atypical antipsychotic
FDA approval: tx of schizophrenia and bipolar I and II depression
MAIN points:
1) unique binding profile with less severe side effects than typical antipsychotics
2) more effective at negative symptoms than other antipsychotics while also targeting positive symptoms
3) potentially lethal for elderly people with dementia
4) antidepressant effects due to serotonin affinity
5) very new drug; new info may emerge

Question 4

cariprazine

Answer 4

TRADE: Vraylar, Reagila, & Symvenu
CLASS: atypical antipsychotic
FDA approval: schizophrenia (psychosis), bipolar I mania and depression, & adjunctive to antidepressants for tx of MDD
MAIN points:
1) highly unique psychodynamic profile considering its partial agonist actions at D2 and D3 receptors
2) effective in treating negative symptoms (schizophrenia) and depressive symptoms (bipolar 1)
3) common side effect is extrapyramidal symptoms across all targeted conditions of tx so monitoring and follow up is important

Question 5

Thioxanthenes are first-generation antipsychotics that are associated with which neurotransmitters?

Answer 5

D2 antagonists; plus, serotonin, norepinephrine, and histamine effects

Question 6

Butyrophenones are first-generation antipsychotics that are associated with a high incidence of which unique side effects?

Answer 6

High incidence of extrapyramidal side effects, particularly Parkinson disease- like symptoms, dystonia, and tardive dyskinesia

Question 7

Which first-generation antipsychotic is available as an inhaled version?

Answer 7

loxapine (Loxitane)

Question 8

Which first-generation antipsychotic induces weight loss?

Answer 8

molindone (Moban)

Question 9

Which first-generation antipsychotic is used more for Tourette’s syndrome?

Answer 9

pimozide (Orap)

Question 10

Which drug was the first second-generation antipsychotic, and what was its primary unique side effect?

Answer 10

clozapine (Clorazil) was the first, came out in 1970s & is still the model for other second gens

agranulocytosis –> reversible with discontinuation of the drug

Question 11

Which second-generation antipsychotic dramatically increases weight but also improves negative symptoms associated with schizophrenia?

Answer 11

olanzapine (Zyprexa)

Question 12

Which second-generation antipsychotic does not have sedative effects due to not binding to histamine receptors?

Answer 12

sertindole (Serlect)

Question 13

Which second-generation antipsychotic is abused more frequently than other antipsychotics due to the sedative and anxiolytic effects?

Answer 13

quetiapine (Seroquel)

Question 14

Which second-generation antipsychotic is used for schizoaffective disorder, produces anxiolytic and antidepressant actions, and is associated with low weight gain?

Answer 14

ziprasidone (Geodon)

Question 15

Which second-generation antipsychotic is associated with lower diabetogenic effects?

Answer 15

amisulpride (Solian)