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NURS 7310 > Pharmacology of antipsychotic agents > Flashcards

Pharmacology of antipsychotic agents Flashcards

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1
Q

All antipsychotics have some propensity to lengthen

A

QTc intervals but these vary widely

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2
Q

What are the four pathways for the dopaminergic system in the brain?

A

Nigrostriatal pathway, mesolimbic pathway, mesocortical pathway, tuberinfundibular pathway

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3
Q

What is the hypothetical function of the Nigrostriatal pathway?

A

Neurons start in the substantia nigra and project to to the striatum for control of motor function. The death of neurons in this pathway can result in Parkinson’s disease.

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4
Q

What is the hypothetical function of the Mesolimbic pathway?

A

Neurons project from the ventral tegmental area to the nucleus accumbens, amygdala, and hippocampus. They play a role in reward and desire, addiction, motivation, and emotional response. If not functioning properly they can cause hallucinations.

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5
Q

What is the hypothetical function of Mesocortical Pathway?

A

Neurons project from the ventral tegmental area to the prefrontal cortex. They are involved in memory and creation of memories. Amnesia and memory issues are a result of inappropriate functioning of this pathways.

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6
Q

What is the hypothetical function of Tuberinfundibular pathway?

A

Neurons start in the hypothalamus and project to the pituitary gland. They play a role in hormonal regulation, maternal behavior and nurturing, pregnancy, and sensory processes. malfunctioning of these pathways can cause hallucinations and interpersonal issues.

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7
Q

CAΨs

A

Conventional antipsychotics

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8
Q

What receptors do conventional antipsychotics affect?

A

non-elective dopamine receptor antagonism

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9
Q

What are the three categories of conventional antipsychotics?

A

phenothiazines, butyrophenones, and thioxanthines

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10
Q

Neuroleptic agents that affect a variety of receptors including dopaminergic receptor sites.

A

What are phenothiazines

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11
Q

Phenothiazides are used to treat…

A

psychosis including schizophrenia; violent agitated, disturbed behavior, and mania secondary to bipolar disorder.

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12
Q

Phenothiazides work by binding to

A

dopamine (D1 and D2), muscarinic, histamine H1, and serotonergic 5HT2 receptors.

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13
Q

Phenothiazides also possess peripheral

A

adrenergic receptor blockage and quinidine-like cardiac effects.

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14
Q

Phenothiazides may do what to seizure thresholds?

A

lower them

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15
Q

What are the signs of clinical toxicity in someone taking phenothiazides?

A

sedation, coma, hypotension, EPS, and cardiac arrythmias

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16
Q

What type of side effects can be seen with phenothiazides?

A

Anticholinergic effects including blurred vision, decreased GI motility, delirium, agitation, hallucination, hyperthermia, tachycardia, and seizures

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17
Q

Name 9 types of phenothiazides?

A

Chlorpromazine, fluphenazine, mesoridazine, perphenazine, prochlorperazine, promazine, thiridazine, Trifluoperazine and triflupromazine

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18
Q

This conventional antipsychotic group is similar to phenothiazides, though probably with less antiadrenergic, anti-histaminic and anticholinergic, and more anti-dopaminergic effects.

A

Butyrophenones

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19
Q

What are the nine types of Butyrophenones?

A

Haloperidol, Droperidol, Bromperidol, Benperidol, Tifluperidol, Melperone, Piamperone, Moperone, Fluanisone

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20
Q

This conventional antipsychotic is more selective D2 agonists and are used most often in children and adolescents. Their side effect profile is like other conventional antipsychotics but also includes restless leg syndrome.

A

Thioxanthenes

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21
Q

What are the seven types of thioxanthenes?

A

Flupentixol, thiotixene, zuclopenthixol, chlorprothixene, lucanthone, clopenthixol, hycanthone

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22
Q

What is a causative factor in the undesirable side effects in conventional antibiotics?

A

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.

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23
Q

When dopamine D2 receptors in the tuberoinfundibular DA pathway are also blocked by conventional antipsychotics it can cause…

A

sedation, motor issues, increased plasma prolactin concentrations (hyperprolactinemia).

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24
Q

Hyperprolactinemia can cause conditions such as

A

galactorrhea (breast secretions), amenorrhea, and may interfere with fertility, demineralization of bones, gynecomastia, sexual dysfunction and weight gain

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25
When dopamine D2 receptors in the nigrostriatal DA pathway are also blocked by conventional antipsychotics this causes
EPS such as akathisia, tremors, dystonia, parkinsonism, tardive dyskinesia
26
The blockade of histamine H1 receptors in conventional antipsychotic drugs causes
weight gain and drowsiness
27
The blockade of a1-adrenergic receptors in conventional antispsychotic drugs causes
cardiovascular side effects such as orthostatic hypotension and drowsiness
28
Low potency conventional antipsychotics require higher doses but
in addition low potency agents tend to have more of the unwanted side effects and are more sedating in general then high potency ones
29
AAΨ
Atypical Antipsychotics
30
What differentiates AAΨ from CAΨ in terms of effectiveness and side effects.
AAΨ have a clinical profile of equal positive symptom antipsychotic actions, but lo EPS and hyperprolactinemia compared to conventional
31
The current atypical antipsychotics as a class are defined as
serotonin-dopamine antagonists with simultaneous serotonin 5HT2A receptor antagonism that accompanies D2 agonism.
32
AAΨ have additional properties that are important such AS
antidepressant actions
33
All antipsychotics are effective for psychotic mania but atypical antipsychotics appear to have greater efficacy for
nonpsychotic mania
34
Which AAΨ has the best anecdotal and clinical evidence for utility in various anxiety disorders
quetiapine
35
What are the three receptors that are blocked by AAΨ that theoretically are responsible for causing sedation?
M1 Muscarinic cholinergic receptors, H1 Histamine receptors, and a1 adrenergic receptors.
36
Clozapine, quetiapine, olanzapine, and iloperidone are all more potent
H1 antagonists than D2 antagonists
37
Only the pines clozapine, quetiapine, and olanzapine have high potency for
muscarinic receptors
38
All AAΨ have at least moderate binding potency to this receptor, but the most potent are clozapine, quetiapine, risperidone, and iloperidone
a1 adrenergic antagonism
39
Which two AAΨ have a high metabolic risk?
Clozapine and olanzapine
40
Which four AAΨ have a medium metabolic risk?
risperidone, paliperidone, quetiapine, iloperidone (weight only)
41
Which four AAΨ have a low metabolic risk?
ziprasidone, aripiprazole, lurasidone, iloperidone (low for dyslipidemia)
42
What are the four parameters that should be tracked when prescribing AAΨ?
weight (BMI), fasting triglycerides, fasting glucose, and blood pressure
43
What are the major factors that determine whether a patient progresses along the metabolic highway to premature death?
unmanageable factors: genetic makeup and age Manageable factors: change in lifestyle Most manageable factors: selection of the antipsychotic
44
How to remember the AAΨ
The pine (peenz), the dones (dohnz), two pips, and a rip, and the others
45
Identify the three pertinent "Pines"
Clozapine (clozaril), Olanzepine (Zyprexa), Quietiepine (Seroquel)
46
The presence of what in Clozapine is linked to its lack of EPS, tardive dyskinesia and hyperprolactinemia?
The presence of serotonin 5HT2A antagonism
47
The gold standard for efficacy in schizophrenia
Clozapine
48
Clozapine may have a particular niche in treating
aggression and violence in psychotic patients
49
Clozapine is the only antipsychotic documented to reduce the risk of this in schizophrenia
suicide in schizophrenia
50
Clozapine may reduce this in some patients with this problem, especially over long treatment intervals.
tardive dyskinesia
51
What is the most important thing to monitor with Clozapine?
Absolute neutrophil count for as long as they are treated with clozapine due to its occasionally fatal complication of agranulocytosis
52
Clozapine may have the greatest efficacy but also the most side effects among the AAΨ. Side effects include:
seizures, sedation, excessive salivation, myocarditis, and the greatest degree of weight gain and cardiometabolic risk
53
Due to its side effects and risks clozapine is considered
NOT first line, but is used when other antipsychotics fail
54
Olanzipine is BLANK potent than clozapine
more
55
Olazipine has LESS
EPS, sedation, prolactinemia
56
Olazipine has significant side effects such as
weight gain, cardiometabolic risks, dyslipidemia (elevating triglycerides) or diabetes,
57
As far as when to prescribe Olanzipine it is considered
second line
58
Quetiapine has a different formation that includes an active metabolite
norquetiapine
59
Quetiapine is BLANK potent than clozapine
MORE
60
Quetiapine has a robust
antidepressant effects
61
Quetiapine should be taken
at night because it is most sedating at its peak delivery shortly after taking it
62
The antipsychotic quetiapine is
an 800 mg ideally XR formulation
63
The antidepressant quetiapine is
300 mg ideally XR formulation
64
The sedative hypnotic quetiapine is
50 mg in the IR formulation
65
Quetiapine is the preferred atypical antipsychotic for patients with
Parkinson's disease who require treatment for psychosis (as is clozapine)
66
Quetiapine has many side effects such as
weight gain, increase in fasting triglycerides, and insulin resistance
67
Name the four "dones" (dohnz)
Risperidone, Paliperidone (invega), ziprasidone (geodon), lurasidone (latuda)
68
This medication is available in a long term depot injectable formulation lasting for 2 weeks, an oral disintegrating tablet, and liquid formaluation
risperidone
69
What side effects are serious concern for risperidone?
it raises prolactin levels even at low doses, weight gain (especially in children), and dyslipidemia
70
This is the active metabolite of risperidone
Paliperidone
71
A big difference between paliperidone and risperidone IS
that paliperidone is eliminated upon urinary excretion and SO has few pharmacokinetic drug interactions and it comes in a sustained-release formulation
72
This AAΨ has a formulation for a depot long term administration of every 4 weeks and is currently the preferred depot AAΨ.
Paliperidone
73
What makes Ziprasidone unique?
It has little or no propensity for weight gain and little issue with dyslipidemia, elevation of fasting triglycerides, or insulin resistance
74
How should ziprasidone be taken?
Twice a day and with food (at least 500 calorie meal)
75
This AAΨ has an intramuscular dosage formulation for rapid use in urgent circumstances
ziprasidone
76
What cardiac complication can be caused by ziprasidone?
QTc prolongation
77
Lurasidone has a high affinity for
5HT7 and 5HT2A
78
What are the benefits of Lurasidone?
little sedation if dosed at night and little weight gain or dyslipidemia (may reverse previous weight gain or dyslipidemia associated with a different AAΨ). It has both antipsychotic and some antidepressant effects.
79
What are the two pips and a rip?
Aripiprazole (abilify), Brexipiprazole (Rexulti), Cariprazine (Vraylar)
80
Aripiprazole is a
D2 partial agonist and 5HT1A partial agonist
81
Aripiprazole is effective in treating
schizophrenia ages 13 and up, mania/mixed mania age 10 and older, and autism related irritability in children ages 6-17
82
Benefits of Aripiprazole include
little or no propensity for weight gain, dyslipidemia, elevation of fasting triglycerides or insulin resistance
83
Brexpiprazole is used to treat
schizophrenia, mania, agitation and psychosis in dementia
84
This AAΨ is still under investigation, but has the interesting potential for development as a weekly, biweekly, or even monthly oral depot
Cariprazine
85
What are the three "other" AAΨ
sulpiride, amisulpride, Sertindole
86
Conventional antipsychotics have lots of side effects due to
dopamine D2 antagonism
87
Atypical antipsychotics have decreased side effects because
D2 antagonism, D2 partial antagonism, 5HT2 antagonism and 5HT1A partial agonism

NURS 7310 (15 decks)

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