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Antipsychotic Drugs - updated
Pharm Assessment 12
42
Pharmacology
Graduate
01/22/2012

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Cards

Term
What are the Positive Symptoms of Psychosis?
Definition
Delusions Hallucinations Disorganized speech Disorganized or catatonic behavior
Term
What are the Negative symptoms of Psychosis?
Definition
Impoverished thoughts Deficits of attention Blunt affect Lack of initiative
Term
What receptors do the Atypical antipsychotics have affinity for? What symptoms do these treat?
Definition
Low D2 Affinity - for + symptoms High 5-HT2 affinity - for - symptoms
Term
What are the Typical antipsychotics largely effective for?
Definition
Treat Positive Symptoms (delusions, hallucinations, disorganization of though and behavior)
Term
What receptors do the Typical Antipsychotics block? What side effects do they have?
Definition
Dopamine D2 Blockers Produce extrapyramidal symptoms Elevate Prolactin Levels
Term
What does the addition of 5HT2A blockade in the Atypical drugs do?
Definition
Reduce EPS improve efficacy for negative symptoms
Term
What are the Typical Antipsycotics?
Definition

Phenothiazenes: Chlropromazine

Thioxanthenes: Thiothixene Butyrophenones&Diphenylbutylpiperidines: Haloperidol

Term
What are the Atypical Antipsychotics?
Definition
Clozapine Risperidone Olanzapine Quetiapine Ziprasidone Aripiprazole
Term
What Typical AP has an Aliphatic Side Chain?
Definition
Chlropromazine (Low Potency)
Term
Which Typical AP has a Piperidine ring in side chain?
Definition
Thiothixene (Lower incidence of EPS)
Term
What Typical AP has the highest potency?
Definition
Haloperidol (Butyrophenones)
Term
What is the only approved agent for use in children and teens?
Definition
Risperidone
Term
What Atypical has low potency?
Definition
Clozapine
Term
What Atypical AP is a D2 partial agonist?
Definition
Aripiprazole
Term
What effect does Aripiprazole have on what receptors? What effect does this have?
Definition
D2 partial agonist (reduces actions of full agonist) 5-HT2A antagonist 5-HT1A partial agonist Lower incidence of side effects
Term
What Atypical has limited EPS at low doses?
Definition
Risperidone
Term
What Atypical has Limited EPS? What receptors does it effect?
Definition
Ziprasidone 5-HT2A, 5-HT1A, 5-HT2C/D2 antagonist
Term
What is Neuroleptic Syndrome?
Definition
Suppression of spontaneous movements and complex behaviors Reduced initiative and interest in environment Decreased manifestations of emotion or affect Psychotic symptoms disappear over time
Term
What antipsychotic agents are more likely to lower the seizure threshold?
Definition
phenothiazines: Chlropromazine
Term
What Antipsychotics are unpredictable when it comes to seizure threshold?
Definition
Butyrophenones: Haloperidol (more likely in predisposed patients)
Term
What is associated with extrapyramidal side effects?
Definition
Decreased Dopamine Activity
Term
How is Prolactin Secretion effected with the antipsychotics?
Definition

Increased: All Typicals Risperidone

 

Little Increase: Clozapine Olanzapine Ziprasidone

 

No Increase: Quetiapine Aripiprazole (decreased?)

Term
What are the clinical consequences of sustained Hyperprolactinemia?
Definition
Sexual Dysfunction Amenorrhea Gynecomastia/Galactorrhea Hypoestrogenism/Osteopenia
Term
What effects do antipsychotics have on the brainstem and chemoreceptor trigger zone?
Definition
Decreased vasomoter reflexes - decreased BP Protect against nausea and vomiting
Term
What antipsychotic may act as an antidiuretic?
Definition
Chlorpromazine
Term
What AP impairs glucose tolerance and decreases insulin release?
Definition
Chlopromazine
Term
What AP cause more orthostatic hypotension? Which cause Less?
Definition

More: Chlorpromazine

 

Less: Haloperidol, Risperidone

Term
What anticholinergic effects can the Antipsychotics have? What agents do these occur in more often?
Definition

Nasal stuffiness Dry mouth Blurred vision More often with Low Potency agents constipation Orthostatic Hypotension

 

 

Term
What are the Extrapyramidal Side effects that AP can cause? What agents do these occure in more often?
Definition
Acute Dystonia Akathesia Parkinsonian Syndrome Neuroleptic Malgnant Syndrome Perioral Tremor Tardive Dyskinesia More often in High Potency Agents
Term
What is Neuroleptic Malignant Syndrome? How is it treated?
Definition
Occurs in first few weeks of treatment Fever, Severe Parkinsonism, Fluctuations Tremor, Autonomic instability, Elevated Creatine Kinase, Myoglobinemia Treat with D2 Agonists: Dantrolene, Bromocriptine
Term
Use of what AP can cause Jaundice in the 2nd-4th week of treatment?
Definition
Chlorpromazine
Term
What AP can cause Blood Dyscrasis?
Definition
Clozapine (Mild leukocytosis, leukopenia, eosinophilia)
Term
What APs is Urticaria or dermatitis common with?
Definition
Phenothiazines: Chlorpromazine (5% on it have it)
Term
What APs cause the most weight gain?
Definition
Clozapine and Olanzapine (all atypicals lead to weight gain)
Term
What is the incidence of Metabolic Syndrome occuring in the Atypical Antipsychotics?
Definition

Olanzapine - High

Quetiapine - Moderate

Risperidone- Moderate

Zisprasidone- Low

Aripiprazole- Low

Term
What causes EPS and Hyperprolactinemia?
Definition
D2 Blockade
Term
What causes Hypotension?
Definition
alpha adrenergic blockade
Term
What causes weight gain?
Definition
histaminic and serotonergic blockade
Term
What are the pharmokinetics for the Antipsychotics?
Definition
Highly Lipophilic Highly protein and membrane bound Accumlates in high blood supply tissues Crosses placenta and Breast milk Peak - 2-4hrs Elimination t1/2 = 20-40hrs
Term
How do the APs disappear from the plasma?
Definition
Rapid redistribution Phase t1/2 = 2hr Slow early elimination Phase t1/2 = 30h
Term
What effects of Physical dependence can develop from the antipsychotics?
Definition
Malaise Difficulty sleeping if aburpt stoppage
Term
What Drug interactions do the Typical Antipsychotics have?
Definition
Inhibit 2D6
(Increase plasma levels of TCAs, SSRIs, other antipsychotics)
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