stahl chapter 5 antipsychotics 151
Actual Answers.
stahl chapter 5 antipsychotics 151
Actual Answers.
Atypical antipsychotics are really misnamed, since they are also used as treatments for both the
_______ and ______ of bipolar disorder, as augmentingagents for treatment-resistant depression, and
"off-label" for various other disorders, such as treatment-resistant anxiety disorders. - ANSWER agents
for treatment-resistant depression, and "off-label" for various other disorders, such as treatment-
resistant anxiety disorders.
"neurolepsis," known as an extreme form of slowness or absence of motor movements as well as
behavioral indifference in experimental animals. The original antipsychotics were first discovered largely
by their ability to produce this effect in experimental animals, and are thus sometimes called
"neuroleptics."
A human counterpart of neurolepsis is also caused by these original (i.e., conventional) antipsychotic
drugs and is characterized by _____3______ - ANSWER psychomotor slowing, emotional quieting, and
affective indifference.
Conventional antipsychotics, also called first-generation antipsychotics or typical antipsychotics, share
the primary pharmacological property of _____antagonism, which is responsible not only for their
antipsychotic efficacy but also for many of their _____ _____.
The therapeutic actions of conventional antipsychotic drugs are hypothetically due to blockade of D2
receptors specifically in the _______ ________ _________(Figure 5-3). This has the effect of reducing
dopamine hyperactivity in mesolimbic dopamine pathway - ANSWER D2,
side effects.
mesolimbic dopamine pathway
All conventional antipsychotics reduce positive psychotic symptoms about equally well in schizophrenia
patients studied in large multicenter trials if they are dosed to block a substantial number of D2
receptors there T/F - ANSWER T
,stahl chapter 5 antipsychotics 151
Actual Answers.
Unfortunately, in order to block adequate numbers of D2 receptors in the mesolimbic dopamine
pathway to quell positive symptoms, one must simultaneously block the same number of D2 receptors
throughout the brain, and this causes undesirable side effects as a "high cost of doing business" with
conventional antipsychotics T/F - ANSWER T
Unfortunately, in order to block adequate numbers of D2 receptors in the mesolimbic dopamine
pathway to quell positive symptoms, one must simultaneously block the same number of D2 receptors
throughout the brain, and this causes undesirable side effects as a "high cost of doing business" with
conventional antipsychotics
Although modern neuroimaging techniques are able to measure directly the blockade of D2 receptors in
the
dorsal (motor) striatum of the nigrostriatal pathway,
for conventional antipsychotics it is assumed that the same number of D2 receptors is blocked in all
brain areas,
including the
ventral limbic area of striatum known as the nucleus accumbens of the mesolimbic dopamine pathway,
the prefrontal cortex of the mesocortical dopamine pathway,
and the pituitary gland of the tuberoinfundibulnar dopamine pathway - ANSWER
All known antipsychotics bind to the dopamine 2 receptor, with the degree of binding determining
whether one experiences therapeutic and/ or side effects.
,stahl chapter 5 antipsychotics 151
Actual Answers.
For most conventional antipsychotics, the degree of D2 receptor binding in the mesolimbic pathway
needed for antipsychotic effects is close to ____%, while
D2 receptor occupancy greater than 80% in the dorsal striatum is associated with extrapyramidal side
effects (EPS) and in the pituitary is associated with hyperprolactinemia.
For conventional antipsychotics (i.e,. pure D2 antagonists) it is assumed that the same number of D2
receptors is blocked in all brain areas. Thus, there is a narrow window between the threshold for
antipsychotic efficacy and that for side effects in terms of D2 binding - ANSWER 80%
D2 receptor occupancy greater than 80% in the dorsal striatum is associated with _________
(dorsal (motor) striatum of the nigrostriatal pathway)
and in the pituitary is associated with ________________.
(pituitary gland of the tuberoinfundibulnar dopamine pathway) - ANSWER extrapyramidal side effects
(EPS)
hyperprolactinemia
Mesocortical dopamine pathway and D2 antagonists.
In untreated schizophrenia, the mesocortical dopamine pathways to dorsolateral prefrontal cortex
(DLPFC) and to ventromedial prefrontal cortex (VMPFC) are hypothesized to be hypoactive, indicated
here by the dotted outlines of the pathway.
This hypoactivity is related to
cognitive symptoms (in the DLPFC),
, stahl chapter 5 antipsychotics 151
Actual Answers.
negative symptoms (in the DLPFC and VMPFC),
and affective symptoms of schizophrenia (in the VMPFC). Administration of a D2 antagonist could
further reduce activity in this pathway and thus not only not improve such symptoms but actually
potentially worsen them. - ANSWER Mesocortical dopamine pathway and D2 antagonists.
Nigrostriatal dopamine pathway and D2 antagonists.
The nigrostriatal dopamine pathway is theoretically unaffected in untreated schizophrenia.
However, blockade of D2 receptors, as with a conventional antipsychotic, prevents dopamine from
binding there and can cause motor side effects that are often collectively termed extrapyramidal
symptoms (EPS). - ANSWER extrapyramidal symptoms (EPS).
Long-term blockade of D2 receptors in the nigrostriatal dopamine pathway can cause upregulation of
those receptors, which may lead to a hyperkinetic motor condition known as tardive dyskinesia,
characterized by facial and tongue movements (e.g., tongue protrusions, facial grimaces, chewing) as
well as quick, jerky limb movements. This upregulation may be the consequence of the neuron's futile
attempt to overcome drug-induced blockade of its dopamine receptors. - ANSWER Tardive dyskinesia.
Tuberoinfundibular dopamine pathway and D2 antagonists.
The tuberoinfundibular dopamine pathway, which projects from the hypothalamus to the pituitary
gland, is theoretically "normal" in untreated schizophrenia.
D2 antagonists reduce activity in this pathway by preventing dopamine from binding to D2 receptors.
This causes prolactin levels to rise, which is associated with side effects such as galactorrhea (breast
secretions) and amenorrhea (irregular menstrual periods). - ANSWER Tuberoinfundibular dopamine
pathway and D2 antagonists.
Actual Answers.
stahl chapter 5 antipsychotics 151
Actual Answers.
Atypical antipsychotics are really misnamed, since they are also used as treatments for both the
_______ and ______ of bipolar disorder, as augmentingagents for treatment-resistant depression, and
"off-label" for various other disorders, such as treatment-resistant anxiety disorders. - ANSWER agents
for treatment-resistant depression, and "off-label" for various other disorders, such as treatment-
resistant anxiety disorders.
"neurolepsis," known as an extreme form of slowness or absence of motor movements as well as
behavioral indifference in experimental animals. The original antipsychotics were first discovered largely
by their ability to produce this effect in experimental animals, and are thus sometimes called
"neuroleptics."
A human counterpart of neurolepsis is also caused by these original (i.e., conventional) antipsychotic
drugs and is characterized by _____3______ - ANSWER psychomotor slowing, emotional quieting, and
affective indifference.
Conventional antipsychotics, also called first-generation antipsychotics or typical antipsychotics, share
the primary pharmacological property of _____antagonism, which is responsible not only for their
antipsychotic efficacy but also for many of their _____ _____.
The therapeutic actions of conventional antipsychotic drugs are hypothetically due to blockade of D2
receptors specifically in the _______ ________ _________(Figure 5-3). This has the effect of reducing
dopamine hyperactivity in mesolimbic dopamine pathway - ANSWER D2,
side effects.
mesolimbic dopamine pathway
All conventional antipsychotics reduce positive psychotic symptoms about equally well in schizophrenia
patients studied in large multicenter trials if they are dosed to block a substantial number of D2
receptors there T/F - ANSWER T
,stahl chapter 5 antipsychotics 151
Actual Answers.
Unfortunately, in order to block adequate numbers of D2 receptors in the mesolimbic dopamine
pathway to quell positive symptoms, one must simultaneously block the same number of D2 receptors
throughout the brain, and this causes undesirable side effects as a "high cost of doing business" with
conventional antipsychotics T/F - ANSWER T
Unfortunately, in order to block adequate numbers of D2 receptors in the mesolimbic dopamine
pathway to quell positive symptoms, one must simultaneously block the same number of D2 receptors
throughout the brain, and this causes undesirable side effects as a "high cost of doing business" with
conventional antipsychotics
Although modern neuroimaging techniques are able to measure directly the blockade of D2 receptors in
the
dorsal (motor) striatum of the nigrostriatal pathway,
for conventional antipsychotics it is assumed that the same number of D2 receptors is blocked in all
brain areas,
including the
ventral limbic area of striatum known as the nucleus accumbens of the mesolimbic dopamine pathway,
the prefrontal cortex of the mesocortical dopamine pathway,
and the pituitary gland of the tuberoinfundibulnar dopamine pathway - ANSWER
All known antipsychotics bind to the dopamine 2 receptor, with the degree of binding determining
whether one experiences therapeutic and/ or side effects.
,stahl chapter 5 antipsychotics 151
Actual Answers.
For most conventional antipsychotics, the degree of D2 receptor binding in the mesolimbic pathway
needed for antipsychotic effects is close to ____%, while
D2 receptor occupancy greater than 80% in the dorsal striatum is associated with extrapyramidal side
effects (EPS) and in the pituitary is associated with hyperprolactinemia.
For conventional antipsychotics (i.e,. pure D2 antagonists) it is assumed that the same number of D2
receptors is blocked in all brain areas. Thus, there is a narrow window between the threshold for
antipsychotic efficacy and that for side effects in terms of D2 binding - ANSWER 80%
D2 receptor occupancy greater than 80% in the dorsal striatum is associated with _________
(dorsal (motor) striatum of the nigrostriatal pathway)
and in the pituitary is associated with ________________.
(pituitary gland of the tuberoinfundibulnar dopamine pathway) - ANSWER extrapyramidal side effects
(EPS)
hyperprolactinemia
Mesocortical dopamine pathway and D2 antagonists.
In untreated schizophrenia, the mesocortical dopamine pathways to dorsolateral prefrontal cortex
(DLPFC) and to ventromedial prefrontal cortex (VMPFC) are hypothesized to be hypoactive, indicated
here by the dotted outlines of the pathway.
This hypoactivity is related to
cognitive symptoms (in the DLPFC),
, stahl chapter 5 antipsychotics 151
Actual Answers.
negative symptoms (in the DLPFC and VMPFC),
and affective symptoms of schizophrenia (in the VMPFC). Administration of a D2 antagonist could
further reduce activity in this pathway and thus not only not improve such symptoms but actually
potentially worsen them. - ANSWER Mesocortical dopamine pathway and D2 antagonists.
Nigrostriatal dopamine pathway and D2 antagonists.
The nigrostriatal dopamine pathway is theoretically unaffected in untreated schizophrenia.
However, blockade of D2 receptors, as with a conventional antipsychotic, prevents dopamine from
binding there and can cause motor side effects that are often collectively termed extrapyramidal
symptoms (EPS). - ANSWER extrapyramidal symptoms (EPS).
Long-term blockade of D2 receptors in the nigrostriatal dopamine pathway can cause upregulation of
those receptors, which may lead to a hyperkinetic motor condition known as tardive dyskinesia,
characterized by facial and tongue movements (e.g., tongue protrusions, facial grimaces, chewing) as
well as quick, jerky limb movements. This upregulation may be the consequence of the neuron's futile
attempt to overcome drug-induced blockade of its dopamine receptors. - ANSWER Tardive dyskinesia.
Tuberoinfundibular dopamine pathway and D2 antagonists.
The tuberoinfundibular dopamine pathway, which projects from the hypothalamus to the pituitary
gland, is theoretically "normal" in untreated schizophrenia.
D2 antagonists reduce activity in this pathway by preventing dopamine from binding to D2 receptors.
This causes prolactin levels to rise, which is associated with side effects such as galactorrhea (breast
secretions) and amenorrhea (irregular menstrual periods). - ANSWER Tuberoinfundibular dopamine
pathway and D2 antagonists.
