conventional antipsychotic drug
DESCRIPTION
M1. 1. H1. conventional antipsychotic drug. D2. Stahl S M, Essential Psychopharmacology (2000). 11-7. Stahl S M, Essential Psychopharmacology (2000). 11-2. pure D2 blocker. Mesocortical pathway. Increase in negative symptoms. Stahl S M, Essential Psychopharmacology (2000). 11-3. - PowerPoint PPT PresentationTRANSCRIPT
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H1M1
D2
1
conventional antipsychotic
drug
11-7 Stahl S M, Essential Psychopharmacology (2000)
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pure D2 blocker
11-2 Stahl S M, Essential Psychopharmacology (2000)
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Increase in negative
symptoms
11-3 Stahl S M, Essential Psychopharmacology (2000)
Mesocortical pathway
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EPSs
11-4 Stahl S M, Essential Psychopharmacology (2000)
Nigrostriatal pathway
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Blockade of receptors in the nigrostriatal dopamine pathway causes them to up-regulate
This up-regulation may lead to tardive dyskinesia
11-5 Stahl S M, Essential Psychopharmacology (2000)
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Motor and mental features of neuroleptic-induced extrapyramidal side effects
Parkinsonism Tremor (resting), rigidity, bradykinesia, masklike facies
Akathisia Restlessness, pacing, fidgeting, shifting from jitteriness, anxiety, irritability, anger, difficulty concentrating
Dystonia Muscle contractions, tongue protrusion, torticollis, opisthotonos, fear, distress, paranoia
Tardive Buccolingual-masticatory movements of irregular
dyskinesia (nonrhythmic) nature; choreiform or athetoid (writhing) movements of fingers, extremities, trunk
Adapted from Ayd 1995; Casey 1995
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D2 receptor prolactin
D2 antagonist
11-32 Stahl S M, Essential Psychopharmacology (2000)
pituitary lactotroph
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Typical antipsychotic drugs: potencies and side effect profiles
Drug Approximate Sedative Hypotensive Anticholinergic Extrapyramidal
dose (mg) effect effect effect effect
Phenothiazines
Chlorpromazine (Thorazine) 100 H H M L
Piperidines
Thioridazine (Mellaril) 95 H H H L
Piperazines
Fluphenazine (Prolixin) 2 M L L H
Perphenazine (Trilafon) 8 L L L H
Trifluoperazine (Stelazine) 5 M L L H
Thioxanthene
Thiothixene (Navane) 5 L L L H
Butyrophenones
Haloperidol (Haldol) 2 L L L H
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5HT2A
D2SDA
11-16 Stahl S M, Essential Psychopharmacology (2000)
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5HT-DA Interactions
11-17 Stahl S M, Essential Psychopharmacology (2000)
Substantia nigra
raphe nucleus
brake
brake
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serotonin neuron
dopamine neuron
Substantia nigra
Raphe
dopamine
5HT2A receptor serotonin
5HT2A receptor
11-18 Stahl S M, Essential Psychopharmacology (2000)
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mesocortical pathway
primary dopamine deficiency
secondary dopamine deficiency
dopamine release
serotonin
SDA
11-27 Stahl S M, Essential Psychopharmacology (2000)
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5HT2A receptor
Nigrostriatal pathway
11-24 Stahl S M, Essential Psychopharmacology (2000)
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5HT7
5HT6
5HT3
5HT2C
5HT1A
M1 H11
2
D1
D3D4
5HT2A
D2
clozapine
11-37 Stahl S M, Essential Psychopharmacology (2000)
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5HT7
1
25HT2A
D2
risperidone
11-39 Stahl S M, Essential Psychopharmacology (2000)
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5HT6
5HT3
5HT2C
M1 H11
D1
D3D4
5HT2A
D2
olanzapine
11-40 Stahl S M, Essential Psychopharmacology (2000)
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5HT7
5HT6
H11
25HT2A
D2
quetiapine
11-41 Stahl S M, Essential Psychopharmacology (2000)
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5HT1DSRI
NRI
5HT7
5HT2C
5HT1A
1
D3
5HT2A
D2
ziprasidone
11-43 Stahl S M, Essential Psychopharmacology (2000)
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Side effects of selected atypical agents
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POSITIVE SYMPTOM PHARMACY
3rd line treatment
2nd line treatment
noncompliant (depot)
1st line treatment
in case of emergency
polypharmacy combos
D2 clozapine
D2
SDA
D2BZ
11-52 Stahl S M, Essential Psychopharmacology (2000)
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Hierarchy of Treatment Goals in Medical Psychotherapy of Schizophrenia
• Acute Phase– Medical/neuropsychiatric assessment– Rapid symptom reduction– Reduce impact of episode on friends, family, housing, activities
• Convalescent Phase– Gain trust/alliance with family/caregivers– Assess and mobilize social supports– Ensure human service needs are met (food, clothing, housing)– Ensure safety and predictability of environment
• Adaptive Plateau– Establish therapeutic alliance/supportive treatment routine– Achieve effective maintenance medication regime
• Stable plateau– Psychoeducation: Promote illness self-management strategies, awareness of relationship
between stress and symptoms– Rehabilitation: Teach adaptive competencies