Antipsychotic Drugs
sometimes called neuroleptics or major tranquilizers
neurolept means affects the brain
are not curative
schizophrenia
chronic psychosis
characteristics
delusions
hallucinations
several different forms
1st generation
block dopamine D2 receptors
receptors part of the reward system
side effects include movement disorders (extrapyramidal symptoms)
no one drug is more effective than another
2nd generation
lower risk of EPS
higher risk of metabolic side effects
diabetes
hypercholesterolemia
act on serotonin and dopamine recepotrs
drug selection
control with minimal side effects
refractory patients
MOA
block D2 receptors
block serotonin receptors
most 2nd generation
block 5-HT2A
chlorpromazine
blocks all
Actions
antipsychotic effects
D2 blockade: mesolimbic (reward center)
positive effects
reduction in hallucinations
reduction in delusions
negative effects (more prominent in 1st generation)
blunted affect
apathy
impaired attention
cognitive impairment
extrapyramidal effects
dystonias
tardive dyskinesia
better in 2nd generations
antiemetic effects
mainly anti-parasympathetic effects
alpha-adrenergic receptor blockade
hypotension
other effects
thermoregulation issues
increased prolactin
general contentment
sedation
Therapeutic uses
schizophrenia
prevention of ausea/vomiting
other uses
tranquilizers
motor tics with Tourette’s
bipolar disorder
adjuncts to antidepressants
Kinetics
oral administration
large Vd
metabolized by CYP450
Adverse effects
significant side effects occur in 80% of patients
low TI
sometimes permanent
extrapyramidal
tardive dyskinesia
permanent
neuroleptic malignant syndrome
others
may lower seizure threshold
may worsen mood
urinary retention
weight gain
seizure
sedation
extrapyramidal
postural hypotension
sexual dysfunction
arrhythmias and sudden cardiac death
dry mouth