Antipsychotics Flashcards
Dopamine Hypothesis
Schizophrenia = increased and unregulated dopamine
Antipsychotics Mechanism
Block postsynaptic D2 receptor, some block DE release
Typicals vs Atypicals
Typical: main risk EPS, reduce + symptoms
Atypical: reduced risk EPS, reduce + and - symptoms
Typical Antipsychotics (4)
Psychos Typically HAte Chlorpromazine Chlorpromazine Phenothiazine Thioridazine Haloperidol
Atypical Antipsychotics
COQ-RAZ
Clozapine Olanzapine Quetiapine Risperidone Ziprasidone Aripiprazole
Antipsychotic Toxicity
"SEA A ENT QT (cutie)" EPS Tardive Dyskinesia Neuroleptic Malignant syndrome Endocrine/metabolic effects Autonomic effects Sedation QT elongation Agranulocytosis (Clozapine)
EPS
Typical»Atypical antipsychotics
- See parkinsonism, akathesia (motor restlessness), dystonia (muscle spasm)
- early-onset side affect (days)
Tardive Dyskinesia
Chorea of lip/buccal muscles
-only long-term development (years), irreversible
Neuroleptic Malignant Syndrome
muscle rigidity, excessive sweating, hypopyrexia (insane body temp), autonomic instability
- life threatening
- occurs early in treatment (days)
Endocrine/metabolic symptoms
Endocrine: From D2 block of tuberoinfundibular pathway- hyperprolactinemia, amennorhea
Metabolic: dyslipidemia, hyperglycemia, diabetes, weight gain
Clozapine (unique side effect, mechanism, treatment ability)
Atypical
-D4 affinity
-Agranulocytosis
Used to treat drug-resistant schizophrenia
Aripiprazole (mechanism and special use)
D2 partial agonist
-will bring DE effect down, but only to 1/4 as partial agonist instead of totally eliminating DE effect like other antipsychotics that inhibit D2 receptors
Antipsychotic drug interactions and half lives
p450 drugs
-various are 3A4, 2D6 metabolized, so watch out for inhibitors (3A4-grapefruit juice, azole antifungals, HIV protease inhibitors. 2D6- bupropion, fluoxetine, paroxetine)
T1/2 ~24h except Quetiapine and Ziprasidone (8h)
