22.1 Pharmacotherapy: Antipsychotics Flashcards
“antipsychotics” used to be called what? (1)
“neuroleptics”
Describe: Overall mechanism of action of antipsychotic (1)
block, to varying degrees, DA activity in target brain pathways
Antipsychotic described for what? (2)
- primarily indicated for psychotic symptoms in: schizophrenia and related disorders, manic episodes, depressive episodes, substance use, medical conditions (i.e. neoplasm)
- other uses: treatment-resistant MDD, severe GAD, complex PTSD, severe OCD, borderline PD, behavioural symptoms of dementia, delirium, Tourette Syndrome, substance abuse in dual diagnosis, Huntington’s disease, ASD, impulse control disorders
- adjunctive management of agitation, aggression, severe anxiety, severe sleep difficulties when sedative-hypnotics are contraindicated
Describe onset: Antipsychotic (2)
- rapid calming effect and decrease in agitation;
- thought disorder responds in 1-4 wk
Name reasons to combine antipsychotics (1)
- no reason to combine two or more antipsychotics
Name effectiveness of antipsychotics (3)
- all antipsychotics are equally effective, except for clozapine (considered to be most effective in treatment-refractory psychosis)
- atypical antipsychotics (second generation) are as effective as typical (first generation) antipsychotics but are thought to have better adverse effect profiles; main difference is lower risk of EPS and TD
- choose a drug to which the patient has responded to in the past or that was used successfully in a family member
Describe duration antipsychotics (2)
- if no response in 4-6 wk, switch drugs
- duration: minimum 6 mo and usually for life in most patients with primary psychotic disorders; variable for other indications
Name Dopamine Pathways Affected by Antipsychotics (4)
- Mesolimbic
- Mesocortical
- Nigrostriatal
- Tuberoinfundibular
Describe effects and associated pathology of this dopamine pathway affected by antipsychotic: Mesolimbic (2)
- Effects: Emotion orginiation, reward
- Associated Pathology: HIGH dopamine causes positive symptoms of schizophrenia (delusions, hallucinations)
Describe effects and associated pathology of this dopamine pathway affected by antipsychotic: Mesocortical (2)
- Effect: Cognition, executive function
- Associated Pathology: LOW dopamine causes negative symptoms of schizophrenia
Describe effects and associated pathology of this dopamine pathway affected by antipsychotic: Nigrostriatal (2)
- Effects: Movement
- Associated pathology: LOW dopamine causes EPS
Describe effects and associated pathology of this dopamine pathway affected by antipsychotic: Tuberofundibular (2)
- Effect: Prolactin hormone release
- Associated pathology: LOW dopamine causes hyperprolactinemia
Describe: Long-Acting Preparations of antipsychotics (6)
- antipsychotics formulated in oil for IM injection
- received on an outpatient basis
- indications: individuals with schizophrenia or other chronic psychosis who relapse because of non- adherence
- should have been exposed to oral form prior to first injection
- dosing: start at low dosages, then titrate every 2-4 wk to maximize safety and minimize side effects
- side effects: risk of EPS, parkinsonism, increased risk of NMS
Describe: Canadian Guidelines for the Treatment of Acute Psychosis in the Emergency Setting (4)
- haloperidol 5 mg IM ± lorazepam 2 mg IM
- loxapine PO 25 mg ± lorazepam 2 mg IM
- olanzapine 2.5-10 mg (PO, IM, quick dissolve)
- risperidone 2 mg (M-tab, liquid)
Compare Typical (First Generation) vs. Atypical (Second Generation) Antipsychotics: Mechanism
- Typical: Block postsynaptic dopamine receptors
- Atypical:
- Block postsynaptic dopamine receptors (D2)
- Block serotonin receptors (5-HT2) on presenaptic dopaminergic terminals, triggering DA release and reversing DA blockade in some pathways
Compare Typical (First Generation) vs. Atypical (Second Generation) Antipsychotics: Pros
- Typical:
- Inexpensive
- Plenty of injectable forms are available
- Atypical:
- Fewer EPS
- Low risk of tardive syndroms
- Mood stabilizing effects
Compare Typical (First Generation) vs. Atypical (Second Generation) Antipsychotics: Cons
- Typical:
- More EPS
- Tardive syndromes long-term
- Not mood stabilizing
- Atypical:
- Expensive
- Few injectable forms available
- Metabolic side effects (weight gain, hyperglycemia, lipid abnormalities, metabolic syndromes)
- Exacerbation (or new onset) of obsessive behaviour
Name: Commonly Used Atypical Antipsychotics (5)
- Risperidone (Risperdal®)
- Olanzapine (Zyprexa®, Zydis®)
- Quetiapine (Seroquel®)
- Clozapine (Clozaril®)
- Ariprazole (Abilify®)