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4. Pharm III > 1- Antipsychotics & Mood Stabilizers/ Bipolar Affective Disorder > Flashcards

1- Antipsychotics & Mood Stabilizers/ Bipolar Affective Disorder Flashcards

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1
Q

Schizophrenia is characterized by hallucinations, delusions, disorganized thinking and emotional abnormalities. The positive sx of schizophrenia are due to what?

A

Overactive DA pathways in the limbic system

(negative sxs: affective behavior, apathetic, withdrawn, anti-social, lack of motivation, depressed)

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2
Q

Hallucinations (auditory > visual), catatonic behavior, disorganized speech and thinking are positive or negative sx of schizophrenia?

A

Positive

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3
Q

T or F: Schizophrenia does not lead to cognitive impairments?

A

FALSE! Cognitive impairments include: distracted, disorganized thought, memory loss

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4
Q

What is the mesolimbic DA pathway?

A

VTA to limbic system

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5
Q

What is the mesocortical DA pathway?

A

VTA to frontal cortex (cognition, emotion)

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6
Q

What is the Nigrostriatal DA pathway?

A

SN to striatum (motor control)

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7
Q

What is the tuberoinfundibular DA pathway?

A

Hypothalamus to pituitary (prolactin)

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8
Q

DA D2 receptors predominate in the mesolimbic system resulting in positive or negative sx?

A

Positive sx

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9
Q

DA D4 receptors predominate in the mesocortical regions resulting in positive or negative sx?

A

Negative sx

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10
Q

What is the MOA for typical antipsychotics?

A

Block DA D2 receptors (targets the mesolimbic sx to alleviate positive sx)

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11
Q

What class of drugs is used to decrease aggression, restlessness, and anxiety?

A

Antipsychotics (typical and atypical)

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12
Q

What class of drugs has a delayed onset of action (~6 wks), has sx persisting for weeks after last admin, and is metabolized by CYP450s?

A

Antipsychotics

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13
Q

What is the effect of prochlorperazine if used in low doses?

A

Antiemetic

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14
Q

SE are very common w/ the antipsychotic class. What are they?

A
  1. Decreased seizure threshold
  2. Endocrine- weight gain, increased prolactin
  3. Dental- xerostomia, bruxism (teeth grinding)
  4. Extrapyramidal sx
  5. Tardive dyskinesia
  6. Neuroleptic malignant syndrome
  7. Autonomic- anticholinergic, a-adrenergic, histamine
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15
Q

What is the tx for EPS sx (tremor, slurred speech)?

A

Tx w/ anticholinergics

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16
Q

Are EPS sx more common w/ typical or atypical antipsychotics?

A

Typical

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17
Q

Neuroleptic malignant syndrome is life threatening. What is the tx?

A

TX w/ Dantrolene

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18
Q

Antipsychotics will interact with anticholinergic drugs resulting in what?

A

More SE

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19
Q

Antipsychotics will interact with Sedative-hypnotics resulting in what?

A

Increased sedation

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20
Q

Antipsychotics will interact with TCAs resulting in what?

A

Seizures and cardiac effects

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21
Q

Why will antipsychotics interact unpredictably with antihypertensive meds

A

Due to alpha-blockade

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22
Q

Antipsychotics will interact w/ what meds?

A
  1. Anticholinergics
  2. Sedative-hypnotics
  3. TCAs 4.

Drugs that induce CYP450s

  1. Antihypertensive
  2. Tobacco (induces CYP450s)
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23
Q

What drug class is Chlorpromazine?

A

Typical antipsychotic

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24
Q

What drug class is Fluphenazine?

A

Typical antipsychotic

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25
What drug class is Haloperidol?
Typical antipsychotic
26
When is chlorpromazine used?
Psychosis associated w/ mania and drugs of abuse, pre-anesthetic
27
What are the SEs of chlorpromazine?
Decreases seizure threshold, sedation, high anticholinergic effects (blurred vision decreased GI motility, inhibition of ejaculation) → low EPS, retinal deposits (browning of vision), postural hypotension, jaundice
28
What is the difference b/w Chlorpromazine and Fluphenazine?
Fluphenazine has less anticholinergic activity → moderate EPS
29
When is Haloperidol used?
Acute situations (very potent)
30
What are the pharmacokinetics of Haloperidol?
Long half life, IV
31
Haloperidol has no anticholinergic activity. What does this mean for EPS?
Lots of EPS
32
What is the MOA for atypical antipsychotics?
Block 5-HT2A and DA2 & DA4 receptors (alleviate negative and positive sx)
33
What areas of the brain does atypical antipsychotics target?
Targets mesocortical & mesolimbic system (alleviate negative and positive sx)
34
What area of the brain does typical antipsychotics target?
Targets mesolimbic systems (alleviates positive sx)
35
What is the MOA for Clozapine?
Block 5-HT2A and D2/4 receptors
36
What are the SEs of Clozapine?
Decreases seizure threshold, hypersalivation, sedation, dizziness, postural hypotension, tachycardia, weight gain
37
What atypical antipsychotic is the last DOC due to agranulocytosis?
Clozapine (blood must be monitored)
38
Are EPS and Tardive dyskinesia common or rare in Clozapine?
RARE
39
What will happen if Clozapine is abruptly discontinued?
Replase
40
What is the MOA for Olanzapine (Zyprexa)?
Atypical psychotic: Block 5-HT2A and DA2/4 receptors
41
What are the other uses for Olanzapine (Zyprexa)?
Bipolar disorder, some anticholinergic activity
42
What are the SEs of Olanzapine (Zyprexa)?
Hyperglycemia, T2DM (“Zyprexia DM”)
43
Are EPS and Tardive dyskinesia common or rare in Olanzapine (Zyprexa)?
RARE
44
What differentiates Olanzapine (Zyprexa) from Clozapine?
Olanzapine (Zyprexa) does not have agranulocytosis
45
What is the MOA for Risperidone?
Atypical psychotic: Block 5-HT2A and DA D2/4 receptors
46
What is the first line drug for psychosis?
Risperidone
47
What are the SEs of Risperidone?
Hypotension Weight gain Insomnia Anxiety Lengthens QT interval
48
Are EPS common or rare in Risperidone?
RARE
49
What is the MOA for Ziprasidone?
Atypical psychotic: Block 5-HT2A and DA D2/4 receptors
50
What are the additional used for Ziprasidone?
Tourettes syndromes Acute mania Some antidepressant activity
51
How is Ziprasidone metabolized?
Metabolized by CYP3A4
52
What are the SE of Ziprasidone?
Prolonged QT interval, sedation, impairs cognitive and motor skills
53
In what population is Ziprasidone given w/ caution?
In pts w/ hx of seizure or drugs that decrease seizure threshold
54
What is the MOA for Aripiprazole?
1. Atypical psychotic: Partial agonist for DA D2/4 and 5-HT1A, Antagonist for 5-HT2A 2. Dopamine system stabilizer
55
What does it mean that Aripiprazole is a DA system stabilizer?
- Activates DA receptors if Dopaminergic tone is low - Blocks DA receptors if dopaminergic tone is high
56
What is the use for Aripiprazole?
Modulates dopamine activity
57
What is Aripiprazole metabolized by?
Metabolized by CYP3A4 and 2D6
58
What are the SEs of Aripiprazole?
Decreased esophageal motility, hyperglycemia, seizures, sedation, increased glucose, postural hypotension
59
Are EPS high or low in Aripiprazole?
LOS
60
What is benefit of Ariprazole vs Ziprasidone and Risperidone?
Ariprazole does not lengthen QT interval
61
What drugs do not increase prolactin?
Ariprazole & Quetiapine
62
What is MOA for Quetiapine?
Atypical psychotic: Block 5-HT2A and DA D2/4 receptors
63
What is the use of Quetiapine?
Promotes sleep onset and maintenance
64
What are the SEs of Quetiapine
Very sedating, dizziness, constipation, xerostomia, postural hypotension, weight gain
65
Are EPS common or rare w/ Quetiapine?
RARE
66
What drugs have do not cause agranulocytosis? (3)
Quetiapine, Olanzapine, Lurasidone
67
What is the MOA for Lurasidone?
1. Atypical psychotic: Block 5-HT2A and DA D2/4 receptors 2. partial agonist for 5-HT1A
68
What is the use of Lurasidone?
Tx of depression associated w/ bipolar disorder
69
What are the SEs of Lurasidone?
Some incidence of agranulocytosis & neutropenia (blood counts should be monitored)
70
What drug has not antihistamine or antimuscarinic effects?
Lurasidone
71
In what disease does a pt alternate b/w manic phases to very deep depression?
Bipolar disorder
72
Bipolar disorder is due to a lack of what NT activity?
GABAergic actvitiy
73
How is Bipolar disorder generally treated?
With a combo of meds
74
What is the MOA for lithium?
suppress 2nd messengers (IP3)
75
What is DOC for tx of bipolar disease?
Lithium
76
Does Lithium have a greater impact on mania or depressed sx?
Mania
77
What medication is absorbed by the gut → not metabolized → excreted by kidneys w/ a t ½ = 24 hrs?
Lithium
78
Where in the kidney is Lithium reabsorbed?
PCT
79
What is the impact of the Lithium being reabsorbed by the PCT?
Competes w/ Na reabsorption
80
If Na decreases, Li absorption increases. What effect does this have on Li?
Lithium toxicity
81
If Na increases → LI absorption decreased. What effect does this have on Lithium?
Increased excretion of Li
82
If Li increased → Na absorption decreases. What effect does this have on Na?
Hyponatremia
83
What does does Li interact with?
1. Antidepressants 2. Diuretics 3. NSAIDS 4. Sodium
84
What is the drug interaction b/w Li and antidepressants?
Increases mania
85
What is the drug interaction b/w Li and diuretics?
Alters salt excretion & Li clearance
86
What is the drug interaction b/w Li and NSAIDs?
Increase Li toxicity (decrease clearance, increase Li uptake)
87
What is the drug interaction b/w Li and Na?
Reduces Li concentration
88
Why does Li have a high # of SEs?
Very small therapeutic window
89
Li can cause what disease states?
Hypothyroidism, Diabetes Insipidus (Li inhibits ADH)
90
What is the TX for Li induced DI?
Tx w/ amiloride (blocks Li into collecting duct)
91
In what population in Li C/I?
Pregnancy
92
What anticonvulsants can be used in the tx of bipolar disorder?
Valproic acid, Gabapentin, Carbamazepine, Lamotrigine
93
What is the use of Valproic acid in the tx of bipolar disorder?
Rapid cycling manic/depressive phases (4-5 x/yr)
94
What is the benefit of using Valproic acid to tx bipolar disorder?
Rapid onset of action (w/ equal or greater efficacy to Li)
95
What is the use of Gabapentin in the tx of bipolar disorder?
Rapid cycling manic/depressive phases (4-5 x/yr)
96
What is the use of Carbamazepine for the tx of bipolar disorder?
Refractory bipolar disorder (used in combo w/ Li)
97
What is the use of Lamotrigine in the tx of bipolar disorder?
Prevention of relapse, depressive state following mania, acute mania
98
Carbamazepine increases the toxicity of what drugs?
Increases toxicity of cimetidine, isoniazid, fluoxetine, erythromycin

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