Antipsychotics Flashcards
Phenothiazine
Chlorpromazine
MOA, Use, and Tox
typical antipsychotics
MOA: D2»5-HT2 antagonist. positive symptoms of psychosis
Use: low clinical potency, inexpensive, used most often
Tox: H1, M1, alpha1 block, parkinson-like effects, akathisia, dystopias, Tardive dyskinesia; deposits in cornea and lens, neuroleptic-malignant syndrome, increased prolactin
phenothiazine/piperazine
fluphenazine (prolixin)
MOA, Use, and Tox
typical antipsychotic
MOA: D2»>5-HT antagonist positive symptoms of psychosis
Use: high clinical potency
Tox: high incidence of tar dive dyskinesias, parkinson-like effects, less autonomic toxicities.
thioxanthenes (nirvana)
MOA, Use, and Tox
typical antipsychotic
MOA: D2»>5-HT antagonist positive symptoms of psychosis
Use: most clinically potent of antipsychotics
Tox: mid-level toxicity of extrapyramidal symptoms, injectable form means less tar dive dyskinesia, less up regulation of D2 receptors. sedation and hypotension.
Butyrophenone Haloperidol (Haldol)
MOA, Use, and Tox
typical antipsychotic
MOA: D2»>5-HT antagonist positive symptoms of psychosis
Use: very potent antipsychotic. for Tourette’s
Tox: most sever extrapyramidal symptoms: Parkinson, akathisia, akinesia, dystonias
Thioridazine MOA, Use, and Tox
typical antipsychotic
MOA: Less D2, more 5-HT2 antagonism
Use: sometimes called atypical in literature. low potency (muscarinic blockade)
Tox: low extrapyramidal effects; ocular toxicity: deposits in retina cause brown vision. Cardiotoxic: T wave, AV block, arrhythmias, HIGHEST RISK FOR PROLONGING QT INTERVAL. sodium channel block
Dantrolene MoA, Use, and Tox.
Muscle relaxant for NMS
MOA: interferes with release of calcium from sarcoplasmic reticulum; ryanodine receptor
Use: skeletal muscle relaxant, neuroleptic malignant syndrome, malignant hyperthermia
Tox: hepatotoxicity, CNS and GI effects
Clozapine MoA, and Tox
atypical antipsychotic
MOA: first atypical drug developed; D4=alpha-1 >5-HT2a >D2=D1
Tox: night time drooling (paradox), weight gain, agranulocytosis: weekly blood counts for the first 6 months of treatment and every 3 weeks thereafter. hypotension
risperidone paliperidone (active metabolite) MOA, and Tox
atypical antipsychotic
MOA: 5-HT2a»_space;>D2; D3 and D4 block
Tox: increased prolactin, hyperlipidemia, hyperglycemia
Olanzapine MOA, Use, Tox
atypical antipsychotic
MOA: blockade of 5-HT2a > H1 > D4 > D2 >alpha-1 >D1
Use: approved in combination with fluoxetine for mania
Tox: less ANS effects. fewer extrapyramidal effects (EPS). weight gain, sedation. metabolic changes like risperidone
Quetiapine MOA, and Tox
atypical antipsychotic
MOA: H1 > a1 >M1,3 > D2 >5-HT2a; D2 blockade, but binds for a short time
Tox: minimal muscarinic block, but high H1 and alpha-1 blockade
Aripiprazole MOA, and Tox
atypical antipsychotic
MOA: partial D2 and 5-HT1a agonist, 5-HT2a antagonist
Tox: weight gain, akathisia
Ziprasidone MOA, Use, and Tox
atypical antipsychotic
MOA: Blocks 5-HT and NE reuptake
Tox: Skin reactions, eosinophilia
Neuroleptic Malignant Syndrome
gradual onset (months-weeks) findings: rigidity decreased reflexes normal pupils drugs: antipsychotic, halogenated anesthetics
Serotonin Syndrome
Abrupt onset Findings: myoclonus and tremor Increased reflexes Dilated Pupil (mydriasis) Drugs: Linezolid, St. John's Wart, "triptans", SSRIs, MAOIs, tricyclic antidepressants.
