Antipsychotics BLOCK III Flashcards
What is psychosis
general term that describes several mental disorders characterized by a defect of lost contact with reality often with hallucinations or delusions
What defines schizophrenia
Schizophrenia: thought disorder characterized by a mix of symptoms such as:
- Hallucinations
- Ideation
- Reality (e.g. delusion)
- Cognition (e.g. loose association)
- Emotions (e.g. flat affect)
What is alogia
Inability to carry on conversation
What is Catatonia
the predominant clinical features involve disturbances in a person’s movement; may exhibit a dramatic reduction in activity, to the point that voluntary movement stops
What is hebephrenia
Disorganized
is thought to be an extreme expression of disorganization syndrome that has been hypothesized to be one feature of a 3-factor model of schizophrenia symptoms, the other factors being; Delusions/hallucinations (reality distortion) Psychomotor poverty (poor speech, lack of spontaneous movement, and blunting emotion)
How do 5-HT blockers effect schizophrenia
Increase the release of DA to alleviate negative symptoms
How do D2 blockers like haloperidol effect schizophrenia
Inhibit DA action and alleviate positive symptoms (hallucinations/ .delusions)
What are the primary NTs involved in Schizo DO
Dopamine
5-hydroxtryptamine (5HT; serotonin)
Glutamate
Is polypharm or monopharm preferred for schizo DOs
Monopharm
What is the APA recommendation for 1* vs 2* gen antipsychotics
Use an atypical antipsychotic first (less risk for EPS)
Patients who prefer or have a history of response to typical antipsychotics may first use typical antipsychotics
Response to medications is NOT immediate, maximal treatment response may take 6 months or longer to be observed
After treatment response observed; maintain current therapy for a minimum of 6 months
What are the 7 clinical uses of Antipsychotics
Antiemetic (Typicals)
Stop Hiccups (Chlorpromazine)
Adjunct Pain Control (off label)
Depression (off label)
Rapid acting Formulations
( acute agitated and disruptive behavior)
Long acting Formulations ( used in pts that lack compliance)
Define EPS
-Dystonia: abnormal tonicity; severe muscle spasm of the head, neck and tongue
-Tardive Dyskinesia (may not be reversible)
Syndrome of involuntary movements of the face, mouth, tongue, trunk and limbs
Occurs in prolonged therapy with drugs that have a high affinity for the D2 receptor (i.e. haloperidol)
-Akathesia (most common EPS)
Desire to be in constant motion (inability to sit still, pacing).
May include feeling of fright, rage, suicide.
Can be confused with anxiety or exacerbation of psychosis
How do we tx EPS
Low dose propranolol and reduce dose of antipsychotics
What is the black box label for antipsychotics
Black Box Warning: increase mortality in elderly patients with dementia-related psychosis
What is the MOA of 1* gen Antipsychotics
Competitive blockers of dopamine receptors D2 in the mesolimbic pathway
Also have activity at histamine, muscarinic, and alpha-receptors
Relatively less effective at controlling the negative symptoms of schizophrenia
How do we treat psuedo Parkinson’s ( drug induced)
Reduce dose
Use an Atypical (2* gen)
Anticholinergic: Trihexyphenidyl or Benzotropine
Antihistamine: diphenhydramine
What are the ADE of 1* gen antipsychotics
QT prolongation Negative/ cognitive s/s Weight gain Postural HOTN Anticholinergic Fx Sedation
What is the most severe ADE of 1* gen antipsychotics
Nueroleptic Malignant Syndrome
Occurs in all agents, but more common with high-potency typical drugs
Symptoms: agitation, confusion, changing levels of consciousness, fever, tachycardia, hypertension, and sweating
Most severe adverse drug event; mortality rate is high and it should be taken seriously
Discontinue the offending agent and provide supportive therapy
What is the relationship of dopamine to prolactin
Dopamine is the major prolactin inhibiting factor so blocking dopamine results in prolactin elevation
Symptoms:
Women: galactorrhea and menstrual irregularities
Men: gynecomastia, sexual dysfunction and decreased fertility
What are the low potency 1* gen antipsychotics
Chlorpromazine and Thioridazine
Lower affinity for dopamine receptors; thus less risk of causing EPS
Possess anticholinergic, antihistaminic, and α-adrenergic blocking properties
Higher rates of sedative, anticholinergic and autonomic adverse effects
What are the high potency 1* gen antipsychotics
Trifluoperazine
Fluphenazine
Haloperidol
High affinity for the dopamine receptors; thus higher rates of extrapyramidal symptoms (EPS)
Less potency at the other receptors
What antipsychotic Tx hiccups
Chlorpromazine
When using chlorpromazine for hiccups, what is the ADE associated with this drug
May cause pigment deposits on the retina and corneal opacity
What are the ADE of Thioridazine
High anti-cholinergic side effects
Highest occurrence of sedation
Black Box Warning: Torsade’s de pointes and sudden death
What is the preferred agent for non-psychotic anxiety
BZDs
What is the clin use of Trifluoperazine
Generalized non-psychotic anxiety
For psychotic patients refusing oral medications what 1* gen med has a clinical indiaction for use
Fluphenazine (IM long acting)
What is the clinical use of Haloperidol
Acute agitation, and Tourette’s
What is the ADE of haloperidol
IV- torsades
EPS and QT elongation
What pts can not receive haloperidol
Parkinson’s Disease
Severe toxic central nervous system depression
comatose states
What is the advantage of 2* gen antipsychotics
Developed to reduce EPS, tardive dyskinesia and improve efficacy
What is metabolic syndrome
Occurs with 2* gen antipsychotics
Weight Gain: check waist circumference at baseline and periodically
Hypertension
Hyperglycemia and/or diabetes mellitus
Lipid abnormalities
How do antipsychotics effect the SZR threshold
Lowers the SZR threshold
Increases risk of SZR
Which 2* gen antipsychotic has the most wt gain, which has the least
Clozapine and Olanzapine have the most
Lurasidone has the least
Which 2* gen antipsychotics have the most hyperglycemia and DM S/s
Clozapine and olanzapine have the most
Lurasidone has the least
Which 2* gen antipsychotics have the most Lipid abnormalities S/s, which have the least
Clozapine and Olanzapine have the most
Lurasidone has the least s
What is the oldest atypical agent, the most effective and is reserved for pts who are resistant to other antipsychotics
Clozapine
What is the only atypical agent indicated to reduce RSK of SI
Clozapine
What is the ADE of Clozapine
Black Box Warning: Agranulocytosis
A reduction in WBC and it increases the risk of serious or fatal infections
Contraindicated if the WBC is <3,500/mm3
Highest during the first 4-6 months of therapy
Monitoring: weekly CBC for first 6 months then every 2 weeks after that while taking the drug
Does Clozapine effect prolactin levels
NO
What is the difference between Olanzapine and clozapine
Olazpaine:
Structurally similar to clozapine and has similar pharmacology
Not associated with agranulocytosis
Olanzapine can be used as an adjunct with what SSRI in the Tx of depression
Fluoxetine
What is the ADE of Olanzapine
Excessive weight gain, sedation, and hypotension compared to the other atypical agents
IV/IM formulations of olanzapine have what risk
IV/IM formulations have a significant risk for respiratory depression; monitor for at least 3 hours post dose
What is the clinical use of Risperidone
Schizophrenia acute psychosis and prevention
Bipolar mania and maintenance therapy
More effective at combating the positive symptoms
Commonly used in children 10-17yo for psychiatric and behavioral disorders
What 2* gen antipsychotics is commonly used in children 10-17 y/o for psych and behavior DO
Risperidone
What 2* gen antipsychotics has the most interacting with prolactin levels
Risperidone
Which 2* gen antipsychotic has the highest EPS RSK
Risperidone
What is paliperidone
Active metabolite of Risperidone
Efficacy is comparable to risperdone
Compared to risperidone, how is paliperidone better of worse with prolactin and EPS
Increased risk of hyperprolactinemia
Compared to risperdone, lower risk of EPS
What is the 2* gen antipsychotic that is a good choice for psychosis with Parkinson’s Dz
Quetiapine
What is the ADE of quetiapine
Very sedating (quetiapine makes you quiet)
Signifigant ortho HOTN,
May causes cataracts
What is the clincal use of Ziprasidone
Tx of Bipolar disorder as monotherapy or adjunct to lithium or valproate
What are the ADE of Iloperidone, a drug used to treat schizophrenia only
Higher risk of orthostatic hypotension and QTc prolongation
Esophageal dysmotility/aspiration
What can you use Lurasidone for
Schizophrenia and bipolar only
What is the route for admin for lurasidone
Oral
How should pts in acute agitation and psychosis be handled
Perform the least offensive or least aggressive things possible to terminate the emergency
Talk the patient down, offer them food or drink, or offer them oral medication (lurasidone)
How should parenteral pharmolocolgy be managed
When very rapid control of agitation is required
Oral treatment is not tolerable
IM or IV injections, then transition patient to oral medication with 24hrs if feasible
Are antipsychotics contraindicated in pregnancy
NO
What is the risk of antipsychotics to mothers/ newborns
Potential risk for EPS signs and withdrawal symptoms in newborns whose mothers were treated with antipsychotics during the 3rd trimester