Pharm: Antipsychotics Flashcards
Which anti-psychotic is indicated for tx of recurrent suicidal behavior?
Clozapine
What are the 5 first-gen. aka typical/conventional antipsychotics?
- Chlorpromazine (low-potency)
- Thioridazine (low-potency)
- Fluphenazine (high-potency)
- Haloperidol (high-potency)
- Thiothixene (high-potency)
What are the 6 second-gen. aka atypical/novel antipsychotics?
- Aripiprazole
- Clozapine
- Olanzapine
- Quetiapine
- Risperidone
- Ziprasidone
What is the MOA of the first gen. anti-psychotics?
Block dopamine (D2) post-synaptic receptors
*so only affects POS sx of schizophrenia, bc less dopamine act
Other than D2-receptors, which other receptors may be blocked by first gen. antipsychotics and how does this correlate with AE’s?
- Muscarinic receptors: dry mouth, constipation, blurred vision…
- Histamine (H1) receptors: sedation
- α1-adrenergic receptors: orthostatic hypotension, dizziness/syncope
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- D2 rec in nigrostriatal pathway – causes EPS
- D2 rec in tuberoinfundibular pathway – causes inc prolactin
What are the dopamine-associated AE’s of the first gen. antipsychotics?
- Hyperprolactinemia (tuberoinfundibular pathway): amenorrhea, galactorrhea, gynecomasta, and ↓ libido
- Extrapyramidal sx’s and Tardive Dyskinesia
What is the only second-gen anti-psychotic that is assoc. with hyperprolactinemia (like the first-gen’s)?
Risperidone
What are the 2 low-potency first gen. antipsychotic agents and what AE’s are they more associated with?
- Chlorpromazine and Thioridazine
- More sedation, hypotension, and ↓ seizure-threshold
What are the 3 high-potency first gen. antipsychotic agents and what AE’s are they more associated with?
- Fluphenazine + Haloperidol + Thiothixene
- More movement (EPS) and endocrine effects (prolactin)
What are the 2 classes + agents used to tx the extrapyramidal sx’s (EPS) of first gen. antipsychotics?
- Anticholinergic agents: benztropine + trihexyphenidyl
- Antihistamine agents: diphenhydramine
Which 2 agents are used for tx of Tardive Dyskinesia (TD) assoc. with first gen. antipsychotics?
Selective VMAT2 inhibitor’s: Valbenazine and Deutetrabenazine
What is the MOA of the second-gen antipsychotic agents?
- Block D2 post-synaptic receptors AND the 5HT2A receptors
- Stronger 5HT2A receptor blockers than D2 receptor blockers
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5HT2A antagonism increases DA transmission in mesocortical pathway –> gets rid of negative sx too
What are some of the common AE’s associated with the second gen. antipsychotics?
Weight gain and Metabolic Sydrome: hyperglycemia/insulin resistance, hyperlipidemia
What are some of the rare AE’s associated with the first and second gen. antipsychotics?
- QTc prolongation and negative inotropic effects –> ↑ risk for women, elderly and those on anti-arrhythmics
- Seizures: with first gen.
Which first generation antipsychotic is more often associated with weight gain, DM, and hypercholesterolemia?
Chlorpromazine
Assc each 2nd gen with it’s worst AE:
- Aripiprazole
- Cariprazine
- Clozapine
- Lurasidone
- Olanzapine/Quietiapine
- Risperidone
- Ziprasidone
- Aripiprazole = none
- Cariprazine = none
- Clozapine = weight gain, hyperchol, sedation, anticholin, ortho hypotension
- Lurasidone = EPS & sedation
- Olanzapine/Quietiapine = weight, hyperchol
- Risperidone = weight, EPS, prolactin
- Ziprasidone = QTc prolongation
Which first gen. antipsychotic is associated with more prolactin elevation, sedation, anticholinergic effects, orthostatic hypotension and a dose-dependent retinitis pigmentosa?
Thioridazine
Which second gen. antipsychotic is more often assoc. with EPS/Tardive Dyskinesia, elevated prolactin, and weight gain/DM?
Risperidone
Which second-gen. antipsychotic is associated with agranulocytosis and requires monitoring of WBC; REMS program?
Clozapine
Before beginning antipsychotics the guidelines recommend determining in all patients which baseline items?
- Serum glucose + Lipids + Weight (BMI)
- Blood pressure
- Waist circumference and Personal/Family hx of metabolic and CV dz
How can non-adherence to antipsychotic meds be managed; which 6 agents can be used?
*test Q*
Manage w/ Long-Acting Injectable Agents (LAIA’s)
- Haloperidol decanoate
- Fluphenazine decanoate
- Risperidone + Olanzapine + Aripiprazole + Paliperidone (ROAP)
Which dopamine pathways cause schizophrenia sx?
Mesolimbic = inc act, positive sx
*motivation, reward
Mesocortical = dec act, negative sx
*cognitive & exec fxn
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Nigrostriatal = dec act, Parkinson dis
Tuberoinfundibular = dec act, connects hypothalamus to pituitary
Which drug is assc w DRESS (drug rxn w eosinophilial and systemic sclerosis)
Olanzapine
