Antipsychotics Flashcards
Chlorpromazine/Thorazine Class Indications MOA SE Char
Typical neuroleptic
Psychosis, mania, schizophrenia
N/V, intractable hiccups
Chiefly D2 dopaminergic receptor site blockade
Also alpha-adrenergic blockade & H1 blockage (anti-histamine effects)
Onset of Parkinsonian symptoms
Tardive dyskinesia
Increased prolactin release (d/t DA blockade) galactorrhea, amenorrhea, infertility (men & women)
SE profile so bad that 2nd generation of antipsychotics were created
Prochlorperazine/ Compazine Class ind MOA SE CHar
Typical neuroleptic
Psychosis
Vertigo
N/V, especially when associated w/ migraines
Primarily H1-histamin receptor antagonist
Also alpha-adrenergic antagonist & D2 dopaminergic antagonist
Significant drowsiness, dry mouth, constipation, urinary retention
Extrapyramidal SE generally seen only when give at high doses over long period of time
Perhaps 10-20x more potent than Chlorpromazine in terms of antipsychotic effects
Less orthostatic hypotension & fewer extrapyramidal signs than chlorpromazine
Better anti-emetic than many other neuroleptics
Lowers seizure threshold
Haloperidol/Haldol
Typical neuroleptic
Psychosis
Tourette’s syndrome
Huntington’s disease
Acute agitated behavior
Chiefly D2 dopaminergic receptor blockade
Chiefly Parkinsonian-like sx & extrapyramidal effects
Tremors common
Neuroleptic malignant syndrome: potentially fatal
“Vitamin H”
Careful administration to reduce excessive sedation & tardive dyskinesia
Less blockade of muscarinic & alpha-adrenergic receptors vs. Chlorpromazine
Clozapine/Clozaril
Atypical neuroleptic
Schizophrenia (especially when other antipsychotics have failed or produced undesirable SE)
Multiple receptor site blockade, greatest effects at D2 & 5HT-2 receptor sites
Relatively diminished extra-pyramidal SE
Agranulocytosis, (1-2%) myocarditis (both potentially lethal)
Clozapine
Clozaril characteristics
PO
Rapid absorption & extensive metabolism
Greatest anti-aggressive effects, more so than any other antipsychotic
Safe use requires weekly blood monitoring for 5 months, then q 4 weeks
Echo every 6 months
3rd line tx d/t SE
D/C if WBC count < 1500
Respiradone/Risperdal
Class Ind MOA SE Char
Atypical neuroleptic
Psychosis
Exact MOA unknown, probably combo of DA & 5HT receptor blockade
Extrapyramidal effects Tardive dyskinesia Constipation Acute sedation Weight gain, hyperglycemia, diabetes Increased stroke risk in elderly
Slow withdrawal to prevent acute psychosis
Metabolism by P450 system – reduce dosage in patients with liver dysfxn
Typically not used in elderly pt
Olanzapine/Zyprexa Class INd MOA SE
Atypical neuroleptic
Schizophrenia (especially when other antipsychotics have failed or produced undesirable SE)
Multiple receptor blockade, greatest effects at D2 & 5HT receptor sites
Severe weight gain, hyperglycemia, diabetes
Increased stroke risk in elderly
Relatively diminished extra-pyramidal SE vs. other neuroleptics
Olanzapine/Zyprexa
Char
PO
Rapid absorption, extensive metabolism
Structurally similar to Clozapine
Higher affinity for 5HT2-R vs. D2-R
Lower affinity for histamine, muscarinic & alpha-adrenergic receptors
US: black box warning – not for elderly patients w/ dementia
Not for patients w/ dementia-related psychosis
30% gain 22 lb or more in 1 year
16% gain 66 lb in 1 year
Aripiprazole/Abilify
CLass
INd
MOA
Atypical neuroleptic
Schizophrenia, bipolar disorder, clinical depression
Partial dopamine agonist
Lithium caebonate/eskalith
class
ind
moa
Lithium salt Bipolar disorder (prophylaxis) Mania (treatment) Schizophrenia Unknown Decrease NEpi transmission Decrease response to glutamate
Lithium carbonate /Eskalith
MOA
MC: impaired concentration capacity d/t reduced renal response to ADH
Polyuria d/t nephrogenic diabetes insipidus (20% patients)
Hypothyroidism 5-35%
Weight gain, cognitive impairment, short-term memory deficits (all -> lack of compliance)
Lithium carbonate /Eskalith
CHar
PO
Renal excretion
Small therapeutic index – blood levels must be frequently checked
Used to be in 7 UP
Signs that levels too high: lethargy, confusion, diarrhea, Abd pain, N/V, ataxia, seere tremors
As levels increase: seizures, cardiotoxicity
Optimal doses: 0.6-1.2 mEq/L
