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Antipsychotic Agents, Relatively low incidence of extrapyramidal effects…
Antipsychotic Agents
First
Generation
Pharmacologic Effects
Antipsychotic
e.g. slowing psychomotor activity (agitation), calming by suppressing hallucinations
-Active against positive effects of psychosis
-Little effect on negative symptoms
Antiemetic
(useful in tx of symptomatic vomiting/nausea)
(historically, prochlorperazine
/Compazine)
Adverse Reactions
Sedation
Tolerance develops to the sedative effect, but not to antipsychotic effect
Extrapyramidal effects
-Extrapyramidal effects exacerbated by withdrawal.
-Can be detrimental for OH!
-(include xerostomia)
Parkinsonism
w/sx of resting tremor, rigidity, & akinesia
Akathisia
increased compulsive motor activity
Acute dystonia
consisting of muscle spasms of the face, tongue, neck, and back
Tardive dyskinesia
Involuntary repetitive body mvmts of tongue, lips, face, jaw
Severe, intermittent pain at TMJ region
Produced by a spasm in the M.O.M.s
In an acute attack, difficult-impossible to open-close jaw
OTHER
Tachycardia, seizures (lower seizure threshold), & anticholinergic effects
Anticholinergic effects from 1st-gen antipsychotics produce blurred vision, XEROSTOMIA, & constipation.
**Esp. significant cuz antichlor effects of other meds pt may be taking may be additive! The anticholinergics (like benztropine- used to treat extrapyramidal sx) are additive, too.
Orthostatic hypotension
Due to depression of central sympathetic outflow & block the peripheral adrenergic receptors (a-sympathetic blockers)
Drug Examples
Medium potency
loxapine
(/Loxitane)
perphenazine
(/Trilafon)
thiothixene
(/Navane)
Low potency
chlorpromazine
(/Thorazine)
thioridazine
(/Mellaril)
High potency
fluphenazine
(/ Prolixin)
haloperidol
(/Haldol)
M.O.A.
Primarily dopamine antagonists
Drug Interactions
CNS Depressants
(benzos, alcohol, general anes., opiods)
Interaction= additive OR potentiating effects
Increased sedation, confusion, dizziness, impaired cognition
Sedation, respiratory depression
Epi
as VC in local
=safe
vasomotor collapse
(acute drop in bp)
=contraindicated
(further decrease in bp)
Second
Generation
Pharmacologic Effects
Antipsychotic
Effective in both positive & negative symptoms
Bipolar
For treatment and rapid control of acute mania sx.
May prevent recurrent episodes of mania & depression
Major depressive disorder
-if antidep insufficient
quetiapine & aripiprazole are FDA-approved for tx of major depressive disorder
Adverse Reactions
Agranulocytosis (=life-threatening blood disorder)
1% of pts who take clozapine= require weekly blood cell count monitoring.
Metabolic effects
Higher risk of hyperglycemia, diabetes, & metabolic syndrome
Tacycardia
Weight gain
notably clozapine, olanzapine, quetiapine
Prolactin elevation
Drug Examples
quetiapine (Seroquel)
risperidone (Risperdal)
clozapine (Clozaril)
cariprazine (Vraylar)
brexpiprazole (Rexulti)
asenapine (Saphris)
aripiprazole (Abilify)
M.O.A.
Action @ multiple receptors
(e.g., @ dopamine, serotonin (5-HT), & NE receptors)
Improved efficacy
Drug Interactions
CNS Depressants
(benzos, alcohol, general anes., opiods)
Increased sedation, confusion, dizziness, impaired cognition
Sedation, respiratory depression
Relatively low incidence of extrapyramidal effects & less likely to cause tardive dyskinesia & neuroleptic malignant syndrome.
NOTE:sx of Psychoses:
positive- hallucinations, sounds, delusions, unwanted thoughts, disorganized behavior, agitation, distorted speech/communication
negative= flat affect, unemotional, apathetic, passive, lack of pleasure, social withdrawal