Antipsychotics Flashcards
positive symptoms of Schizophrenia
Hallucinations, delusions, disorganized speech and behavior
negative symptoms of Schizophrenia
apathy, lack of motivation, difficulty speaking
cognitive symptoms of Schizophrenia
deficits in working memory, central processing, social cognition, problem solving
conventional; typical (Neuroleptic) effects of antipsychotic drugs
- induce EPS
- increase circulating [Prolactin]
- block D2 receptors (and many other receptors)
- sedation and autonomic effects
atypical effects of antipsychotic drugs
- less EPS
- block DA and 5-HT1,5-HT2,6,7 receptor subtypes;some have partial agonist activity; variable blockade of other receptors
- variable effect of [prolactin]
effects of low potency antipsychotics
more sedation and autonomic effects
effects of high potency antipsychotics
more EPS; less sedation and hypotension
clozapine has greater usefulness in treating
resistant pts
AE of atypical antipsychotics
-hypotension, seizures, weight gain, hyperglycaemia, hyperlipidemia
what are the 4 major dopamine pathways
- Nigrostriatal (pars compacta; Parkinsons)
- Mesocortical; mesolimbic (frontal cortex)
- tuberoinfundibular (-prolactin)
- chemoreceptor trigger zone (emesis)
what are pharmacologic effects of typical agents
- CNS (sedation; dec. seizure threshold)
- extrapyramidal rxn (acute dystonia, parkinsonism, Akathisia, Tardive dyskinesia)
- Neuroleptic malignant syndrome
what is neuroleptic malignant syndrome
- relatively rare rxn associated w/ antipsychotic agents, especially parenterally administered high-potency drugs
- mortality rate ~5%
what is neuroleptic malignant syndrome associated w/
hyperthermia, diffuse muscular rigidity, autonomic dysfunction and fluctuating levels of consciousness
what lab values does neuroleptic malignant syndrome alter
- elevate creatine kinase
- leukocytosis
- elevate hepatic transaminase
- increase myoglobin
which antipsychotics are long-acting
Fluphenazine Decanoate
Haloperidol Decanoate
Risperidone
who are long acting antipsychotics useful in
noncompliant pts
what autonomic effects do antipsychotics have
- hypotension (orthostatic) from alpha receptor blockade
- anticholinergic effects (dry mouth, tachcardia, blurred vision, urinary retention, constipation, confusion/toxic delirium)
- impairment of thermoregulation
cardiac effects of antipsychotics
- direct negative inotropic and quinidine-like effects (phenothiazines)
- Q-T prolongaion: thioridazine, mesoridazine, pimazide, haloperidol, ziprasidone)
neuroendocrine effects of antipsychotics
-hyperprolactinemia which may cause galactorrhea (women) and gynecomastia (men)
other AE of antipsychotics
- edema, weight gain; delayed ovulation, menstruation, amenorrhea; sexual dysfunction
- rare ophthalmic, hepatic, and hematologic effects
clozapine
-minimal risk of extrapyramidal effects
what SE have been reported with Clozapine
- akathisia, muscle stiffness, NMS
- agranulocytosis, benign hyperthermia, seizures, hypersalivation; weight gain; sedation, dizziness
- tachycardia; orthostatic hypotension
what are the atypical antipsychotics
- Risperidone
- Olanzapine
- Quetiapine
- Ziprasidone
- Aripiprazole
- Asenapine
- Iloperidone
SE of Risperidone
movement disorders; sexual dysfunction
SE of Olanzapine
weight gain; glucose intolerance; hyperlipidemia
SE of Quetiapine
cataracts
SE of Ziprasidone
prolong QT interval; less weight gain
what are the label warnings for Atypicals
-increased risk of weight gain, glucose intolerance/diabetes mellitus, and hyperlipidemia
pharmacokinetics of antipsychotics
- half life 10-35 hrs
- metabolized by hepatic oxidation
Asenapine and Olanzapine are primarily cleared by
glucuronidation
what are the drug interactions of antipsychotics
- block a-recptors
- potentiate CNS (and respiratory depression)
- may potentiate cardiovascular depression
- competitive inhibitor of CYP2D6 and/or 3A4
clinical uses of antipsychotics
- acute phase schizophrenia
- maintenance phase schizophrenia
other psychiatric uses
Mania
Schizoaffective disorder
Delusional disorder
Major depression with psychotic features
Delirium, brief reactive psychoses, sensory deprivation syndromes, rage reactions
Organic mental syndromes
Pervasive developmental disorder (autism)
Agitated behavior associated w/mental retardation or dementia
Borderline personality disorder
what effects do antipsychotics have in the elderly
-increase morality
what are non-psychiatric uses of antipsychotics
Tourette's syndrome Chorea of Huntington's disease Ballism Intractable hiccups Emesis
