Antipsychotics Flashcards
hallucinations, delusions, disorganized speech, agitation, behavioral dyscontrol caused by change in what neurotransmitter and receptor?
increased dopamine binding to post synaptic D2-receptors (positive symptoms)
apathy, avolition, alogia + cognitive deficits caused by change in what neurotransmitter and receptor?
decreased dopamine binding to D1-receptors (negative symptoms)
D1 or D2 sx easier to tx?
D2 (positive) - all antipsychotic drugs target D2
class of antipsychotic:
Haloperidol
Chlorpromazine
Fluphenazine
typical agents - “azine”
class of antipsychotic:
Aripiprazole
Brexpiprazole
Clozapine
Olanzapine
Quetiapine
Paliperidone
Risperidone
Ziprasidone
atypical agents - “piprazole” and “apine” and “idones”
Main difference between typical and atypical antipsychotics
Reduction in movement‐disorder SE’s (EPS) with atypical drug development - esp high potency fluphenazine and haloperidol
Four receptors that atypicals can block
D1, D2, D4, 5H-T
***2 Atypical agents also a partial agonist at presynaptic (D2 /D3 & 5HT1A)
apripirazole and brexpiprazole
1 Atypical agent’s metabolite that also potently blocks NERT
(norquetiapine) quetiapine
Typical Antipsychotic agent that is low potency - drug name and this means?
Chlorprimazine
-More sedation, hypotension and seizure‐threshold reduction - less mvmt disorders.
AE of high potency typical antipsychotics - and name of two drugs
fluphenazine, haloperidol
-EPS movement disorder if >80% D2 receptor occupancy
Three receptors, other than Dopamine Receptors, that may be blocked by antipsychotics and side effects.
o Muscarinic (anti-cholinergic) = dry mouth, constipation, urinary retention, blurred vision, sedation o Histaminic (H1 primarily) = sedation o Alpha‐adrenergic (α1 & α2) = orthostatic hypotension and impotency
**Three possible (anti-cholinergic) drugs to treat acute Dystonia/Akathisia/Dyskinesia/Parkinsonism‐like symptoms (EPS) caused by Typical Class
Anticholinergic agents
• Diphenhydramine (Benadryl)
• Benztropine (Cogentin)
• Trihexyphenidyl
Severe side effect of clozapine. So monitor what?
agranulocytosis
-monitor WBC
Define Neuroleptic Malignant Syndrome
Rare but potentially‐fatal, severe Parkinson’s‐like movement disorder
• Autonomic instability, Stupor, Hyperpyrexia, Muscle rigidity, Altered mental status
• More common with injectable, high‐potency Typical agents but possible with all agents
Four classic Atypical Class side effects. So monitor what?
- Seizure threshold reduction
- Stroke
- Metabolic syndrome - wt gain, hyperglycemia, hyperlipidemia
- QT prolongation/ECG changes
Monitor: Baseline serum glucose, lipids, weight, blood pressure, and when possible, waist circumference and personal and family histories of metabolic and CV disease.
A dementia patient taking Olanzapine, Paliperidone, Risperidone - major risk increase?
stroke
**EPS:
worst
best
worst: haloperidol
best: atypical class
**Weight gain:
worst
best
worst - clozapine, olanzapine "pines" best - All of the typical class and the "piprazoles"
**Stoke risk:
worst
best
worst - olanzapine, paliperidone, risperidone
best - any other, esp typicals
**ECG changes
worst
best
worst - chlorpromazine (typical), fluphenazine (typical), ziprasidone (atypical)
best - “apine”, “piprazole”
four drugs that affect 5HT1 receptors
atypicals - ariprazole, brexpiperazole, clozapine, ziprasidone
Used for?
• Haloperidol decanoate
• Fluphenazine decanoate
Ri Ol Ar Pa • Risperidone • Olanzapine pamoate • Aripiprazole • Paliperidone palmitate
Non‐adherence can be managed with long‐acting injectable agents (LAIAs) (every 1‐4 weeks, depending on agent, dose & patient factors)
Psychotic with anti‐suicidal‐thoughts/behaviors
Major adverse effect.
clozapine
SE: agranulocytosis - monitor WBC