Antipsychotics Flashcards
Chlorpromazine
- Phenothiazine, aiphatic typical.
- Low-medium potency, sedative, with pronounced anticholinergic side effects.
Clozapine
- Atypical; blocks D4 and 5-HT2 receptors, with litte effect on D2. Also muscarinic antagonist.
- Improves positive symptoms even in patients not helped by other drugs; most efficacious.
- Improves negative symptoms.
- Lowers seizure thresholds more than other antipsychotics.
- Can cause fatal agranulocytosis, so requires monitoring.
Thioridazine
- Phenothiazine; peridine typical.
- Low potency, sedative, with fewer extrapyramidal and anticholinergic actions
Olanzapine
- Related to clozapine; potent 5-HT2 antagonist, with some D1 and D2 antagonist action, and some D4 action. –Less seizure incidence than clozapine and no risk of agranulocytosis.
- Weight gain and diabetes-related adverse events.
- There have been reports of olanzapine abuse.
- Can also be used for augmentation during depression.
Thiothixene
- Thioxanthine typical.
- Non-nitrogen containing analogs of the phenothiazines; pharm is similar.
Haloperidol
-Butyrophenone derivative; not chemically related to phenothiazines but pharm. similar to high-potency piperazine derivatives.
Pimozide
- Potent neuroleptic; many side effects.
- Approved for treatment of Tourette’s in patients where haloperidol doesn’t work.
Risperidone
- Atypical; combined D2 and 5-HT2 antagonist.
- Greater reductions in negative symptoms and less EPS than traditional psychotics.
- Less seizure activity and less antimuscarinic activity than clozapine.
- Active metabolite is paliperidone; both available as IM depot prep.
Quetiapine
- Structurally related to clozapine; similar to risperidone and olanzapine in effects on schizophrenia symptoms and side effects, with shorter half-life.
- Approved for augmentation in depression. Some reports of abuse.
Ziprasidone
- Atypical.
- 5-HT2 and D2 antagonist; may have 5-HT1a agonist activity.
- No weight gain.
Aripiprazole
- Atypical.
- A partial D2 agonist and 5-HT2 antagonist.
- Also approved for augmentation/adjunct therapy for depression.
Clonazepam
-Used for initial control of manic symptoms.
Lithium Carbonate
- Monovalent of the lightest alkali metal.
- One of the few psychotherapeutic drugs that has no behavior effects in normals. Blocks manic behavior.
- Sodium levels affect lithium levels; increases Na excretion causes clinically significant increase in lithium levels (watch out for thiazide diuretics, losses of fluid/electrolytes). ACEI and ARBs also can raise lithium levels.
- Side effects: fatigue, muscle weakness, tremor, GI symptoms, slurred speech and ataxia, serious toxicity (impaired consciousness, rigidity and hyperactive deep reflexes, coma).
- Narrow therapeutic window.
- Should be used with caution in pregnant women.
- Used to treat mania and prevent bipolar recurrence. May be useful in preventing recurrences of unipolar depression in some patients. Also used for schizoaffective disorder and cluster headaches.
Valproic Acid
- Lithium alternative.
- Used as first line drug in bipolar disorder; sedating.
Actions of antipsychotic drugs
- Decrease psychotic behavior
- Sedation
- Extrapyramidal effects (dystonia, akathisia, parkinsonism have early onset, tardive dyskinesia develops later)
- Anticholinergic activity (dry mouth, blurred vision, urinary retention)
- Orthostatic hypotension
- Neuroendocrine effects due to DA receptor blockade
- Allergic effects
- Decreased seizure threshold
- Weight gain.