NR 546 week 3 Assignment; Antipsychotics Medications Table 1&2 Updated 2023.

NR 546 week 3 Assignment; Antipsychotics Medications Table 1&2 Updated 2023. Drug name Indication Target symptoms: state if positive or negative effect Potency (if noted. receptor occupancy if noted ) Neurotransmitter(s) affected Half-life (T1/2), metabolism (CYP 450 enzyme) Notable side effects (associate to pathway or NT) Typical antipsychotics (conventional) Haloperidol Blocks dopamine 2 receptors, reducing positive symptoms of psychosis and possibly combative, explosive, and hyperactive behaviors Blocks dopamine 2 receptors in the nigrostriatal pathway, improving tics and other symptoms in Tourette’s syndrome. Decanoate half-life approximately 3 weeks Oral half-life approximately 12–38 hours Acute blockade of dopamine 2 receptors in the striatum can cause drug-induced parkinsonism, dystonia, or akathisia Chronic blockade of dopamine 2 receptors in the striatum can cause tardive dyskinesia By blocking dopamine 2 receptors in the pituitary, it can cause elevations in prolactin By blocking dopamine 2 receptors excessively in the mesocortical and mesolimbic dopamine pathways, especially at high doses, it can cause worsening of negative and cognitive symptoms (neuroleptic-induced deficit syndrome). Blocking alpha 1 adrenergic receptors can cause dizziness, hypotension, and syncope Thioridazine Blocks dopamine 2 receptors, reducing positive symptoms of psychosis Metabolized by CYP450 2D6 Acute blockade of dopamine 2 receptors in the striatum can cause drug-induced parkinsonism, dystonia, or akathisia. Chronic blockade of dopamine 2 receptors in the striatum can cause tardive dyskinesia By blocking dopamine 2 receptors in the pituitary, it can cause elevations in prolactin By blocking dopamine 2 receptors excessively in the mesocortical and mesolimbic dopamine pathways, especially at high doses, it can cause worsening of negative and cognitive symptoms (neuroleptic-induced deficit syndrome) Blocking muscarinic cholinergic receptors can cause dry mouth, blurred vision, urinary retention, constipation, and paralytic ileus Antihistaminic actions may cause sedation, weight gain Blocking alpha 1 adrenergic receptors can cause dizziness, hypotension, and syncope Thiothixene Blocks dopamine 2 receptors, reducing positive symptoms of psychosis Commonly prescribed for schizophrenia and bipolar disorder Initial elimination half-life approximately 3.4 hours Terminal elimination half-life approximately 34 hours Acute blockade of dopamine 2 receptors in the striatum can cause drug-induced parkinsonism, dystonia, or akathisia Chronic blockade of dopamine 2 receptors in the striatum can cause tardive dyskinesia. By blocking dopamine 2 receptors in the pituitary, it can cause elevations in prolactin By blocking dopamine 2 receptors excessively in the mesocortical and mesolimbic dopamine pathways, especially at high doses, it can cause worsening of negative and cognitive symptoms (neuroleptic-induced deficit syndrome) Blocking muscarinic cholinergic receptors can cause dry mouth, blurred vision, urinary retention, constipation, and paralytic ileus Antihistaminic actions may cause sedation, weight gain Blocking alpha 1 adrenergic receptors can cause dizziness, hypotension, and syncope. Fluphenazine Blocks dopamine 2 receptors, reducing positive symptoms of psychosis Commonly prescribed for Bipolar disorder Mean half-life of oral formulation approximately 15 hours Mean half-life of intramuscular formulation approximately 6.8–9.6 days Acute blockade of dopamine 2 receptors in the striatum can cause drug-induced parkinsonism, dystonia, or akathisia Chronic blockade of dopamine 2 receptors in the striatum can cause tardive dyskinesia By blocking dopamine 2 receptors in the pituitary, it can cause elevations in prolactin. By blocking dopamine 2 receptors excessively in the mesocortical and mesolimbic dopamine pathways, especially at high doses, it can cause worsening of negative and cognitive symptoms (neuroleptic-induced deficit syndrome) Blocking muscarinic cholinergic receptors can cause dry mouth, blurred vision, urinary retention, constipation, and paralytic ileus Antihistaminic actions may cause sedation, weight gain Blocking alpha 1 adrenergic receptors can cause dizziness, hypotension, and syncope Mesoridazine Mesoridazine is used to treat the symptoms of schizophrenia and reduce restlessness, anxiety, and tension. It can also reduce hyperactivity and uncooperativeness. mesoridazine, as with other phenothiazines, acts indirectly on reticular formation, whereby neuronal activity into reticular formation is reduced without affecting its intrinsic ability to activate the cerebral cortex. In addition, the phenothiazines exhibit at least part of their activities through depression of hypothalamic centers. Neurochemically, the phenothiazines are thought to exert their effects by a central adrenergic blocking action. Half life 24- 48hrs drowsiness dry mouth nausea vomiting diarrhea constipation restlessness headache Chlorpromazine Indications Schizophrenia (oral) Severe behavioral problems associated with oppositional defiant disorder or other disruptive behavioral disorders, or for attention deficit hyperactivity disorder (ADHD) in pediatric patients who show excessive motor activity with accompanying conduct disorders (oral, intramuscular for acute, severe agitation in hospitalized patients) Acute psychosis (intramuscular) Nausea, vomiting (oral, rectal, intramuscular, intravenous) Acute intermittent porphyria (oral, intramuscular) Tetanus (intramuscular, adjunct). Intractable hiccups (oral, intramuscular, Half-life approximately 8–33 hours Acute blockade of dopamine 2 receptors in the striatum can cause drug-induced parkinsonism, dystonia, or akathisia Chronic blockade of dopamine 2 receptors in the striatum can cause tardive dyskinesia By blocking dopamine 2 receptors excessively in the mesocortical and mesolimbic dopamine pathways, especially at high doses, it can cause worsening of negative and cognitive symptoms (neuroleptic-induced deficit syndrome) Blocking muscarinic cholinergic receptors can cause dry mouth, blurred vision, urinary retention, intravenous) Bipolar disorder Restlessness and apprehension before surgery Blocks dopamine 2 receptors, reducing positive symptoms of psychosis and improving other behaviors Combination of dopamine D2, histamine H1, and cholinergic M1 blockade in the vomiting center may reduce nausea and vomiting constipation, and paralytic ileus Antihistaminic actions may cause sedation, weight gain Blocking alpha 1 adrenergic receptors can cause dizziness, hypotension, and syncope.