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Psychiatry Pharmacology > Antipsychotic Drugs > Flashcards

Antipsychotic Drugs Flashcards

1
Q

PRIMARY DRUGS

A 
CHLORPROMAZINE (Typical)
FLUPHENAZINE  (Typical)
HALOPERIDOL  (Typical)
ARIPIPRAZOLE (Atypical)
CLOZAPINE (Atypical)
OLANZAPINE (Atypical)
RISPERIDONE (Atypical)
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2
Q

Secondary Drugs

A 
perphenazine (Typical)
thiothixene (Typical)
paliperidone (Atypical)
quetiapine (Atypical)
ziprasidone (Atypical)
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3
Q

Phenothiazenes =

A

zine

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4
Q

2nd Generation drugs with highest potential for CYP-interactions (3A4/2D6)

A

Risperidone, Aripiprazole, Quetiapine, Ziprasidone

Think RAQZ

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5
Q

2nd Generation Antipsychotics that are most likely to cause Diabetes & Weight Gain

A

Clozapine

Olanzapine

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6
Q

2nd Generation Antipsychotics most likely to cause EPS

A

Risperidone

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7
Q

2nd Generation Antipsychotics least likely to cause QTc Prolongation

A

Aripirazole

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8
Q

2nd Generation Antipsychotics most likely to cause QTc Prolongation

A

Ziprasidone

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9
Q

2nd Generation Antipsychotics that cause Elevated

Prolactin

A

Palperidone

Risperidone

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10
Q

Definition of Psychosis

A

A symptom of a major mental disorder in which:
 Personality is seriously disorganized
 Contact with reality is usually impaired
 Ability to think, perceive, and judge is impaired (often with delusions and/or hallucinations)
 Ability to communicate & relate to others is impaired
 Ability to cope with the environment is impaired
 Ability to meet the ordinary demands of life is impaired

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11
Q

Diagnostic Criteria for Schizophrenia

Characteristic Symptoms:

A

2 or more, each present for a significant proportion of the time for 1 month (or less if treated)
 Delusions
 Hallucinations
 Disorganized Speech
 Grossly disorganized or catatonic behavior
 Negative symptoms (affective flattening, alogia, or avolition)

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12
Q

Diagnostic Criteria for Schizophrenia

Include:

A

 Social/Occupational Dysfunction
 Signs of the disturbance present for 6 months or longer
 Schizoaffective and mood disorders have been ruled out
 Substance abuse and general medical conditions have been ruled out
 In presence of autism, hallucinations or delusions present for over 1 month

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13
Q

Idiopathic Psychosis

Positive Symptoms

A

 Delusions
 Hallucinations
 Disorganized speech
 Disorganized or catatonic behavior

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14
Q

Idiopathic Psychosis

Negative Symptoms

A

 Impoverished thoughts
 Deficits of attention
 Blunt affect
 Lack of initiative

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15
Q

Receptors Clinical potency correlates with

A

in vitro inhibition of D2 receptor binding.

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16
Q

Receptors Other

A

Muscarinic, alpha-adrenergic, histamine H1 and serotonin 5-HT2 receptors

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17
Q

Receptors Atypical antipsychotics

A

 Low D2 affinity

 High 5-HT2 affinity

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18
Q

Treatment of Psychosis

Antipsychotics Factors:

A

 Typical vs. Atypical

 Low Potency vs. High Potency

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19
Q

Typical Antipsychotics: Definition

A

 Dopamine D2 blockers
 Produce extrapyramidal symptoms (EPS)
 Elevate prolactin (PRL) levels
 Equally effective but differ in potency/side effects
 Largely effective for positive symptoms (e.g., delusions, hallucinations, disorganization of thought and behavior)

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20
Q

Atypical Antipsychotics: Definition

A

 Share D2 and 5HT2A antagonism in common
 Addition of 5HT2A blockade may:
- reduce EPS
- improve efficacy for negative symptoms e.g., withdrawal, flat affect, paucity of thought,
avolition (poor initiation of goal directed
behavior)

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21
Q

Antipsychotics

A

 Phenothiazines
 Thioxanthenes
 Butyrophenones (phenylbutylpiperidines)
& Diphenylbutylpiperidines

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22
Q

Chlropromazine Structure

A

Aliphatic side chain

Low potency

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23
Q

Thiothixene Structure

A

Piperidine ring in side chain

Lower incidence of EPS

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24
Q

Fluphenazine & Perphenazine Structure

A

Piperazine group in side chain

Potent

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25
Butyrophenones example
 Haloperidol |  High potency
26
Clozapine Type/Potency
 Low potency  Atypical antipsychotic  Olanzapine and Quetiapine
27
Risperidone Receptor/Beneifits
```  5-HT2/D2 antagonist  Limited EPS at low doses  Only approved agent for use in children and teens  Paliperidone • Active metabolite ```
28
Aripiprazole Receptor/Potency
 D2 partial agonist  Reduces actions of full agonist  5-HT2A antagonist, 5-HT1A partial agonist  Lower incidence of side effects
29
Ziprasidone Receptor/Side Effects
 5-HT2A, 5-HT1A, 5-HT2C/D2 antagonist |  Limited EPS
30
Neuroleptic Syndrome Define:
 Suppression of spontaneous movements and complex behaviors  Reduced initiative and interest in environment  Decreased manifestations of emotion or affect  Psychotic symptoms disappear over time
31
CNS Effects Cerebral Cortex
```  Minimal adaptive changes in dopamine system  Can lower seizure thresholds  More likely with low potency phenothiazines  Butyrophenones unpredictable  More likely in predisposed patients ```
32
CNS Effects Basal Ganglia
 Suggested that decreased dopamine activity associated with extrapyramidal side effects (EPS)  Antipsychotics consistently increase dopamine metabolism  Antipsychotic effects not thought to occur here  Initially increase dopamine metabolism, synthesis and firing rate  Diminishes with time
33
CNS Effects Limbic System
 Thought to be site of antipsychotic effects |  Anticholinergics do not block therapeutic effect
34
CNS Effects Hypothalamus
 Increased prolactin secretion  Little tolerance  Avoid in patients with established breast carcinoma
35
Effects on Prolactin Secretion
``` Interference with dopamine secretion or action leads to an increase in serum prolactin All Typicals Increased Risperidone Increased Clozapine Little Increase Olanzapine Little Increase Ziprasidone Little Increase Quetiapine No Increase Aripiprazole No Increase (decrease?) ```
36
Clinical Consequences of Sustained Hyperprolactinemia
Sexual dysfunction Amenorrhea Gynecomastia/Galactorrhea Hypoestrogenism/Osteopenia?
37
CNS Effects Brainstem
 Little effect on respiration  Decreased vasomotor reflexes  Occurs at low doses
38
CNS Effects Chemoreceptor Trigger Zone
 Protect against nausea and vomiting elicited by activation of dopamine receptors  Occurs at low doses
39
Autonomic Nervous System
Complex and unpredictable
40
Renal System
Chlorpromazine may be antidiuretic
41
Hepatic System
 No characteristic effects |  May be toxic in patients with liver disease
42
Endocrine System Chlorpromazine Side Effects
 Impairs glucose tolerance |  Decreases insulin release
43
Endocrine System Drugs that Increased risk of Type II diabetes
Clozapine, risperidone, aripiprizole, | ziprasidone, olanzepine and quetiapine
44
Cardiovascular System Effects
 Direct effects on heart and vessels  Indirect effects via CNS and ANS  Mild orthostatic hypotension - More so with chlorpromazine, thioridazine - Less so with haloperidol, loxapine, risperidone - Tolerance develops
45
May increase acetylcholine turnover
Mainly basal ganglia
46
Inverse relationship between antimuscarinic | potency and
EPS
47
Toxic Reactions/Side Effects
```  High Therapeutic Index  Anticholinergic Effects - Nasal stuffiness - Dry mouth - Blurred vision - Constipation - Cardiovascular - Orthostatic Hypotension ```
48
Extrapyramidal Side Effects
```  Acute Dystonia  Akathesia  Parkinsonian Syndrome  Neuroleptic Malignant Syndrome  Perioral Tremor  Tardive Dyskinesia ```
49
Acute Dystonia Symptoms/Treatment
``` Symptoms  Muscle spasms  Facial Grimacing  Torticollis: stiff neck  Oculogyeric crisis Treatment  Anticholinergic antiparkinsonian agents ```
50
Akathesia Symptoms/Treatment
``` Symptoms  Strong subjective feelings of distress or discomfort often referred to the legs  "Ants in the pants" Treatment  Decrease dose  Add antiparkinsonian agent  Antianxiety agent or propranolol ```
51
Parkinsonian Syndrome Symptoms/Treatment
``` Symptoms  Akinesia  Mask facies  Decreased arm movement  Rigidity  Tremor Treatment  Anticholinergic antiparkinsonian agents  Amantadine ```
52
Neuroleptic Malignant Syndrome
```  Rare  Fever  Severe Parkinsonism with catatonia  Fluctuations in coarse tremor intensity  Autonomic instability  Elevated creatine kinase  Myoglobinemia  High mortality (10%) ```
53
Neuroleptic Malignant Syndrome Treatment
Treatment  Immediate cessation of antipsychotic  Supportive care  Dantrolene or bromocriptine may help
54
Perioral Termor
 Rare  Rabbit syndrome  Treat with anticholinergic agents  Stop neuroleptic
55
Tardive Dyskinesia
 Stereotyped, repetitive, quick choeriform (tic-like) movements of face eyelids (blinks or spasms), mouth (grimaces), tongue, extremities or trunk  No adequate treatment  Discontinue antipsychotic  Symptoms fade with time
56
Side Effects Jaundice
 Occurs during 2nd-4th week with chlorpromazine  Hypersensitivity reaction  Mild  Change agents
57
Side Effects Blood Dyscrasis
 Mild leukocytosis, leukopenia, eosinophilia  Especially important when using clozapine  Leukopenia may be forewarning of impending agranulocytosis  Weekly white blood cell counts
58
Side Effects Skin Reactions
```  Urticaria or dermatitis  5% of patients on chlorpromazine  More common with phenothiazines  Occur in first 8 weeks  Skin clears with discontinuation  Photosensitivity ```
59
Side Effects Weight Gain
 Clozapine, Olanzapine more likely  Risperidone, Quetiapine, intermediate risk  Ziprasidone, Aripiprazole, Asenapine less likely  Increased risk of Type II diabetes mellitus, hypertension and hyperlipidemia  Children/Adolescents  Atypicals lead to weight gain
60
Metabolic Syndrome
 Abdominal obesity  Atherogenic dyslipidemia (blood fat disorders — high triglycerides, low HDL cholesterol and high LDL cholesterol)  Elevated blood pressure  Insulin resistance or glucose intolerance  Prothrombotic state (e.g., high fibrinogen or plasminogen activator inhibitor–1)  Proinflammatory state (e.g., elevated C-reactive protein)
61
Incidence of Metabolic Syndrome on Atypical Antipsychotics
``` Drug Incidence Olanzapine High Quetiapine Moderate Risperidone Moderate Zisprasidone Low Aripiprazole Low ```
62
EPS & hyperprolactinemia—
D2 blockade
63
Hypotension—
alpha adrenergic blockade
64
Sedation—
histaminergic blockade
65
Weight gain—
histaminic & serotonergic blockade
66
Anticholinergic (e.g., dry mouth)—
muscarinic blockade
67
Sexual side effects—
serotonergic, muscarinic, noradrenergic and D2 (via prolactin) blockade
68
Pharmacokinetics
 Oral absorption erratic  Bioavailability increase 4-10x when given intramuscularly  Highly lipophilic  Highly protein and membrane bound  Accumulates in high blood supply tissues  Crosses placental barrier and enters breast milk  Biological effect usually lasts 24 hr  Give entire daily dose at once
69
Metabolism
```  Oxidation main route - Hepatic microsomal oxidases and conjugation  Most metabolites inactive  Exceptions - 7-OH-chlorpromazine - Several N-methylated metabolites of phenothiazines - Paliperidone - Dehydroaripirazole ```
70
Tolerance/Physical Dependence
 Not addicting  Some physical dependence  Malaise, difficulty sleeping if abrupt stoppage  Tolerance develops to sedative effects over days to weeks
71
Drug Interactions Typical Antipsychotics
 Metabolized at 2D6 and 3A4  Do not induce P 450 enzymes  Many inhibit 2D6 - Raise levels of many TCAs and SSRIs - Raise levels of many other antipsychotics  Theoretically vulnerable to inducers and inhibitors of 2D6 and 3A4, though little is known about this in vivo

Psychiatry Pharmacology (2 decks)

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