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Commonly Prescribed Antipsychotics
Antipsychotics - MOA
20
Psychology
Graduate
06/14/2012

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Term

aripiprazole (abilify)

atypical antipsychotic

third generation, sometimes included as a second generation, mood stabilizer

 

MECHANISM OF ACTION

Definition

da partial agonist - *partial agonism at da 2 receptors

  • reduces da output when da concentrations are high, thus improving + symptoms and mediating antipsychotic actions.
  • increases da output when concentrations are low, thus improving cognitive, --, and mood symptoms.
  • actions at da 3 receptors could theoretically contribute to efficacy.
  • partial agonism at 5ht1a receptors may be relevant at clinical doses.
  • blockade of 5ht2a may contribute at clinical doses to cause enhancement of da release in certain brain regions, thus reducing motor se's and possibly improving cognitive and affective sx's. 

 

Term

aripiprazole (abilify)

dopamine partial agonist, atypical antipsychotic, third generation, sometimes included as a second generation, also a mood stabilizer

 

USUAL DOSING RANGE

Definition

  15-30mg/day

 

Term

aripiprazole (abilify)

dopamine partial agonist, atypical antipsychotic, third generation, sometimes included in second generation, also a mood stabilizer

 

APPROVED FOR:

Definition

schizophrenia (ages 13 and older)

maintaining stability in schizophrenia

acute mania/mixed mania (ages 10 and older)

bipolar maintenance

depression (adjunct)

autism related irritablilty in children (ages 6-17)

Term

aripiprazole (abilify)

dopamine partial agonist, atypical antipsychotic, third generation, sometimes included as a second generation, also a mood stabilizer

 

DOSAGE FORMS

Definition

tablets:  2mg, 5mg, 10mg, 15mg, 20mg, 30mg

orally disintegrating tablet:  10mg, 15mg

oral solution:  1mg/ml

injection:  9.75mg/1.3ml

Term

aripiprazole (abilify)

dopamine partial agonist, atypical antipsychotic, third generation, sometimes included as a second generation, also a mood stabilizer

BEST AUGMENTING COMBOS FOR PARTIAL RESPONSE
Definition
valproic acid (valproate, divalproex, divalproex er), other mood-stabilizing anticonvulsants (carbamazepine, oxcarbazepine, lamotrigine), lithium, benzodiazepines.
Term

aripiprazole (abilify)

dopamine partial agonist, atypical antipsychotic, third generation, sometimes included as a second generation, also a mood stabilizer

TEST PRIOR TO STARTING
Definition
wt, ht, bmi, waist circumference, bp, fasting plasma glucose, fasting lipid profile, personal and family hx of dm, obesity, dyslipidemia, htn, and cvd.
Term

aripiprazole (abilify)

dopamine partial agonist, atypical antipsychotic, third generation, sometimes included as a second generation, also a mood stabilizer

MONITOR AFTER STARTING
Definition
bmi q3mo, then quarterly
consider fasting triglycerides monthly, for several months for those at high risk of metabolic complications
bp, fasting plasma glucose, fasting lipids within 3 months, then annually but earlier and more frequently for patients with dm or who have gaind >5% of initial wt. *be vigilant for dm ketoacidosis, patients with hx of leucopenia/neutropenia should have cbc first few months.
Term

aripiprazole (abilify)

dopamine partial agonist, atypical antipsychotic, third generation, sometimes included as a second generation, also a mood stabilizer

SIDE EFFECTS
Definition
by blocking alpha 1 adrenergic recptors, it can cause dizziness, sedation, and hypotension.
partial agonist actions at da2 receptors in the striatum can cause motor side effects
partial agonist actions at da2 receptors can also cause nausea, occasional vomiting, and activating se's
Term

aripiprazole (abilify)

dopamine partial agonist, atypical antipsychotic, third generation, sometimes included as a second generation, also a mood stabilizer

HOW TO DOSE
Definition
initial approved recommendation is 10-15mg/day; max approved dose 30mg/day
oral solution doses can be substituted for table doses on a mg-per-mg basis up to 25mg (pts receiving 30mg tab should receive 25mg solution)
Term

aripiprazole (abilify)

dopamine partial agonist, atypical antipsychotic, third generation, sometimes included as a second generation, also a mood stabilizer

HOW TO STOP
Definition
slow down-titration (over 6-8wks) especially when simultaneously beginning a new antipsychotic
rapid discontinuation could theoretically lead to rebound psychosis and worsening sx's.
Term

aripiprazole (abilify)

dopamine partial agonist, atypical antipsychotic, third generation, sometimes included as a second generation, also a mood stabilizer

PHARMACOKINETICS
Definition
metabolized primarily by CYP450 2D6 and CYP450 3A4
mean elimination half-life 75hrs and 94hrs for major metabolite.
Term

aripiprazole (abilify)

dopamine partial agonist, atypical antipsychotic, third generation, sometimes included as a second generation, also a mood stabilizer

DRUG INTERACTIONS
Definition
ketoconazole and possibly other CYP450 3A4 inhibitors such as nefazodone, fluvoxamine, and fluoxetine may increase plasma levels.
carbamazepine and possibly other inducers of CYP450 3A4 may decrease level plasma levels.
quinidine and possibly other inhibitors of CYP450 2D6 such as paroxetine, fluoxetine, and duloxetine may increase levels.
may increase levels of antihypertensives
may antagonize levodopa, dopamine agonists
Term

aripiprazole (abilify)

dopamine partial agonist, atypical antipsychotic, third generation, sometimes included as a second generation, also a mood stabilizer

PREGNANCY
Definition
risk category c
psychotic sx's may worsen during pregnancy and some form of tx may be necessary
may be preferable to anticonvulsant mood stabilizers if tx is required during pregnancy
Term

aripiprazole (abilify)

dopamine partial agonist, atypical antipsychotic, third generation, sometimes included as a second generation, also a mood stabilizer

PRIMARY TARGET SYMPTOMS
Definition
+ sx's psychosis
-- sx's of psychosis
cognitive sx's
unstable mood
aggressive symptoms
Term
chlorpromazine (thorazine)
conventional antipsychotic, neuroleptic, phenothiazine, dopamine 2 antagonist, aniemetic
APPROVED FOR
Definition
schizophrenia, nausea, vomiting, restlessness and apprehension before surgery, acute intermittent porphyria, manifestations of manic type of manic-depressive illness, tetanus (adjunct), intractable hiccups, combativenesss and/or explosive hyperexcitable behavior (in children), hyperactivity, and pscyhosis.
Term
chlorpromazine (thorazine)
conventional antipsychotic, neuroleptic, phenothiazine, dopamine 2 antagonist, aniemetic
MOA
Definition
blocks dopamine 2 recptors, reducing + sx's 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.
Term
chlorpromazine (thorazine)
conventional antipsychotic, neuroleptic, phenothiazine, dopamine 2 antagonist, aniemetic
BEST AUGMENTING COMBOS
Definition
addition of a mood-stabilizing anticonvulsant such as valproate carbamazepine, or lamotrigine may be helpful in both schizophrenia and bipolar mania
augmentation with lithium in bipolar mania may be helpful
addition of a benzodiazepine, especially short-term for aggitation
Term
chlorpromazine (thorazine)
conventional antipsychotic, neuroleptic, phenothiazine, dopamine 2 antagonist, aniemetic
TEST PRIOR TO STARTING
Definition
wt, ht, bmi, fasting plasma glucose, ldl cholesterol, and triglycerides
Term
chlorpromazine (thorazine)
conventional antipsychotic, neuroleptic, phenothiazine, dopamine 2 antagonist, aniemetic
MONITOR AFTER STARTING
Definition
wt, ht, bmi, fasting triglycerides monthly for several months in patients at high risk for metabolic complications and when initiating or switching antipsychotics
bp in elderly
elevated prolactin levels
pts with hx of drug induced leucopenia/neutropenia should have cbc frequently in beginning of tx and during first few months.
Term
chlorpromazine (thorazine)
conventional antipsychotic, neuroleptic, phenothiazine, dopamine 2 antagonist, aniemetic
SIDE EFFECTS
Definition
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