Flashcards in Antipsychotics Deck (34)
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:
typical agents - "azine"
class of antipsychotic:
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
Typical Antipsychotic agent that is low potency - drug name and this means?
-More sedation, hypotension and seizure‐threshold reduction - less mvmt disorders.
AE of high potency typical antipsychotics - and name of two drugs
-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
• Diphenhydramine (Benadryl)
• Benztropine (Cogentin)
Severe side effect of clozapine. So monitor what?
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
-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?
best: atypical class
worst - clozapine, olanzapine "pines"
best - All of the typical class and the "piprazoles"
worst - olanzapine, paliperidone, risperidone
best - any other, esp typicals
worst - chlorpromazine (typical), fluphenazine (typical), ziprasidone (atypical)
best - "apine", "piprazole"
four drugs that affect 5HT1 receptors
atypicals - ariprazole, brexpiperazole, clozapine, ziprasidone
• Haloperidol decanoate
• Fluphenazine decanoate
Ri Ol Ar Pa
• Olanzapine pamoate
• 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.
SE: agranulocytosis - monitor WBC
In comparing typical antipsychotics, what is associated with skeletal muscle rigidity, tremor at rest, uncontrollable restlesness, and spastic torticollis?
haloperidol (this is EPS)
Woman has schizophrenia. Current tx is a typical agent, experiencing amenorrhea and galactorrhea. What antipsychotic agent would decrease severity?
**Prolactin (amenorrhea and glactorrhea dt D effects)
worst - typical class
best - atypical class
blurred vision, dry mouth, mydriasis - what receptor are these SE of?
**drug induced orthostatic hypotension
chlorpromazine or clozapine (*many SE - WBC, seizures)
(least-fluphenazine, haloperidol, paliperidone, ziprasidone)