Antipsychotic Drugs Flashcards
Dopamine hypothesis of schizophrenia
- Blocking D2 receptors in CNS (mesolimbic frontal system) alleviates psychotic symptoms
- Drugs that increase dopaminergic activity aggravate schizophrenia
- Schizophrenic patients have increased dopamine receptor density
Relationship between clinical efficacy of antipsychotics and affinity for D2 receptors
Higher affinity for D2 receptors = lower dose needed to achieve efficacy
EPS
Extrapyramidal symptoms- reversible neurologic effects
- Movement disorders:
- Parkinson-like syndrome
- Akathisia
- Dystonia
Akathisia
Motor restlessness- part of EPS
Dystonia
Muscle spasms- part of EPS
What do you treat acute dystonia with?
Diphenhydramine (antihistamine + anticholinergic) OR muscarinic blocking agents
Tardive dyskinesia
Choreoathetoid movements of lips/buccal cavity
-effect of chronic use of antipsychotics
Treat tardive dyskinesia
- Discontinue drug
- Eliminate drugs with anticholinergic action
- Add diazepam
Neuroleptic malignant syndrome
Most severe adverse effects of antipsychotics
- muscle rigidity, excessive sweating, autonomic instability, lead pipe rigidity, altered mental status, fever, rhabdomyelisis
- can persist for days even after neuroleptic is stopped
Treat neuroleptic malignant syndrome
Dantrolene (muscle relaxant at ryanodine receptor) + bromocriptine (dopamine agonist)
Are antipsychotics lipophilic or lipophobic?
Lipophilic- readily enter CNS
High Vd- long duration
Chlorpromazine
Typical antipsychotic- low potency
-corneal deposits
Thioridazine
Typical antipsychotic- low potency
- retinal deposits
- strongest autonomic and anti-muscarinic effects
Haloperidol
Typical antipsychotic- high potency
- blocks D2 the most –> high EPS
- weakest autonomic and muscarinic effects
Fluphenazine
High potency typical antipsychotic