1
Q
List the classical antipsychotics
A
- Chlorpromazine (Thorazine®)
- Prochlorperazine (Compazine®)
- Fluphenazine (Prolixin®)
- Haloperidol (Haldol®)
2
Q
what class is Clozapine (Clozaril®) in
A
atypical antipsychotics
3
Q
what class is Olanzapine (Zyprexa®) in
A
atypical antipsychotics
4
Q
what class is Quetiapine (Seroquel®) in
A
atypical antipsychotics
5
Q
what class is Aripiprazole (Abilify®) in
A
atypical antipsychotics
6
Q
what class is Risperidone (Risperdal®) in
A
atypical antipsychotics
7
Q
what class is Ziprisadone (Geodon®) in
A
atypical antipsychotics
8
Q
what class is Lithium (Eskalith®) in
A
mood stabilizer
9
Q
what class is Valproic acid (Depakene®) in
A
mood stabilizer
10
Q
what class is Carbamazepine (Tegretol®) in
A
mood stabilizer
11
Q
what class is Gabapentin (Neurontin®) in
A
mood stabilizer
12
Q
what class is Lamotrigine (Lamictal®) in
A
mood stabilizer
13
Q
What are examples positive symptoms
A
- hallucinations, delusions, catatonic behavior, disorganized speech and thinking
14
Q
positive symptoms are due to what neurological pathway
A
- over active dopamine pathway in limbic system: mesolimbic
15
Q
what are some examples of negative symptoms
A
- affective behavior, apathetic, withdrawn, anti-social, lack of motivation, depression
16
Q
negative symptoms are due to what neurological pathway
A
- under-active dopamine pathways in frontal cortex: Mesocortical
17
Q
the mesolimibic pathway goes from where to where? what is it responsible for?
A
- VTA (ventral tegmental area) to limbic system
- emotion
18
Q
The mesocortical system travels from where to where? what is it responsible for
A
- VTA (ventral tegmental area) to frontal cortex
- cognition and emotion
19
Q
the Nigrostriatal pathway travels from where to where? what is it responsible for
A
- Substantia nigra to striatum
- motor control
20
Q
the Tuberoinfundibular pathway travels from where to where? what is it responsible for
A
- hypothalamus to pituitary
- Prolactin release
21
Q
MOA of the “classical” antipsychotics (Neuroleptics)? what dopamine system do they target? What symptoms do they relieve
A
- block dopamine D2 receptors
- targert mesolimbic system
- alleviate positive symptoms
22
Q
MOA of the “atypical” antipsychotics? what dopamine system do they target? What symptoms do they relieve
A
- block 5-HT2A and dopamine receptors
- target mesocortical and mesolimbic system
- alleviate both negative and positive symptoms
23
Q
Dopamine D2 are highly concentrated in what area of brain
A
limbic system
- The potency for blocking the D2 receptor correlates well with the efficacy at relieving the “positive” symptoms of schizophrenia
24
Q
effects of antipsychotics takes how long
A
6 weeks
25
general effects specific to Prochlorperazine (Compazine®)
antiemetic
26
most (classical and atypical) drugs also block what receptors
* muscarininc
* a-adrenergic
* histamine
\*\*brain and periphery
27
antipsychotic medications have what effect on seizures
decrease seizure threshold
28
endocrine side effects of antipsychotic medications
* weight gain
* increased prolactin secretion
29
anticholinergic, anti a-adrenergic, and anti histamine effects of antipsychotic medications
* anticholinergic: dry mouth, blurred vision, tachycardia, constipation
* anti a-adrenergic: postural hypotension
* anti histamine effects: sedation
30
What are extrapyramidal symptoms
* parkinson's like symptoms : tremor, rigidity, dyskinesia, rocking (akathisia), pacing, restlessless, anxiety, dystonia
31
why do antipsychotic medications cause extrapyramidal symptoms
* D2 antagonists block not only DA receptors in the limbic system, but also those in the **nigrostriatal system** (substantia nigra, striatum).
* **imbalance of striatal DA and ACh**
32
how are extrapyramidal symptoms treated
* treat with **anticholinergics** such as **Benztropine (Cogentin)** to restore ACh/DA balance
33
which class of antipsychotics tend to cause more EPS symptoms
* classical antipsychotics tend to cause more EPS than atypicals
* the higher the degree of anticholinergic activity of the drug, the less likely to cause EPS
34
15-25% of patients will have tardive dyskinesia. What is this
* uncontrollable, jerky movements of face and limbs
* occurs late in disease following long-term tx
* discontinue drug
35
which two antipsychotic drugs are the least likely to cause tardive dyskinesia
* Clozapine
* Olanzapine
36
What is Neuoleptic Malignant syndrome? what is it caused by
* life threatening, starts with muscle rigidity, fever, changes in BP and HR
* caused by **block** of **Dopamine D2 receptors** in the striatum and hypothalamus
37
What can be used to treat Neuoleptic Malignant syndrome
* **Dantrolene (dantrium)**
38
MOA of classical antipsychotics
* block Dopamine D2 receptors
39
classical antipsychotics are metabolized by
* CYP450s (2D6 and 3A4)
* high first pass metabolism
40
effects of classical antipsychotics last for how long
* weeks after last administration
* bad for pt compliance
41
Chlorpromazine has what incidence of EPS? why?
* low incidence of EPS
* High anticholinergic activity
42
MOA of Chlorpromazine
* blocks DA D2 receptors
* blocks a-adrenergic receptors and ACh
43
side effects of Chlorpromazine
* anticholinergic: blurred vision, dry mouth, constipation
* **decreased** **sz** **threshold**
* **retinal deposits:**"browning of vision"
44
How does Fluphenazine compare to Chlorpromazine
* both block DA D2 receptors
* has less anticholinergic activity -\> more likely to cause EPS
45
MOA of Haloperidol "Vitamin H"
* **potent blocker of DA D2 receptor**
* also affinity for DA D1, 5-HT2, and a1 receptors
46
when is Haloperidol "Vitamin H" used
* used frequently in **acute setting (ER)**
* can be **injected**
47
main side effect of Haloperidol "Vitamin H"
* **extrapyramidal symptoms**
* **no anticholinergic acitivity**
* don't use long term
48
MOA of Clozapine
* **blocks 5-HT2A **and **DA D4 receptors**
* some affinity for D2
49
what happens if Clozapine is discontinued abruptly
* rapid relapse
* unique!
50
side effects of Clozapine
* **agranulocytosis**
* ****makes it drug of **last choice**
* blood must be monitored
* EPS and tardive dyskinesia are rare
51
MOA of Olanzapine
* blocks **5-HT2A receptors** and **DA D4 and D2** **receptors**
* improves positive and negative symptoms
* used in tx of bipolar
52
side effects of Olanzapine
* **hyperglycemia**, type II diabetes
* extrapyramidal symptoms rare
53
first line drug for psychosis
Risperidone
54
MOA of Risperidone
* blocks **5-HT2A** and **DA D2 receptors**
* improves both **positive** and **negative** symptoms
* **no significant effect** on DA neurotransmission in **nigrostriatal pathway**
55
MOA of Ziprasidone
* blocks **5-HT2A** and **DA D2 receptors**
* some **antidepressant activity**
* 5HT1A agonist, inhibit 5 HT reuptake
56
unique side effects of Ziprasidone
* prolongs QT interval
* sedation
* Hyperprolactinemia
57
MOA of Quetiapine
* blocks **5-HT2A** and **DA D2 receptors**
58
side effects of Quetiapine (Seroquel)
* **very sedating\*\*\***
* ****used to promote sleep onset and maintenance
* **does not elevate prolactin**
59
MOA of Aripiprazole (abilify)
* **dopamine system stabilizer**
* ****dopaminergic tone is low -\> DA receptors are activated
* dopaminergic tone is high -\> DA receptors are blocks
* **partial agonist** for **DA D2** and **5-HT1A** receptors
* **antagonist** for **5-HT2A**
60
unique side effect of Aripiprazole
* decreases esophageal motility
61
what is thought to be a cause of bipolar affective disorder
* a lack of **GABA**ergic activity
62
DOC for bipolar affective disorder
* lithium
63
metabolism of Lithium
* **No metabolism**
* excreted by kidneys
64
MOA of Lithium
* suppress 2nd messengers (IP3)
* may increase ACh, NE, and DA
65
how is lithium reabsorbed?
* reabsorbed by the **proximal tubule** in the kidney
* **competes with sodium** for re-absorption
* Na+ decreases -\> Li+ absorption increases -\> **toxicity**
* Li+ increases -\> Na+ absorption decreases -\> **hyponatremia**
66
Lithium has a small therapeutic window. what plasma levels are associated with side effects and toxicity
* **Plasma levels \> 2 mEq/L** -\> N/D, _tremor_
* **Plasma levels \> 2.5 mEq/L** -\> confusion, slurred speech, sz, renal failure, cardiac arrhythmias
67
patients taking lithium can get **diabetes insipidus**. why? what is a tx?
* Li+ inhibits ADH
* treat with **amiloride (**blocks entry of Li+ into collecting duct)
68
lithium is contraindicated in
pregnancy
69
What happens when lithium + benzodiazepines or antipsychotics
SAFE
70
lithium + NSAIDs -\>
* **increase Li toxicity**
71
if patient can not tolerate lithium for bipolar, what is the next drug of choice
* **valproic acid**
* best used for **rapid cycling manic/depressive phases**
72
side effects of valproic acid
* surgical bleeding (dental)
* teratogenic
73
Which two anticonvulsants are useful for rapid cycling manic/depressive phases of bipolar disorder
1. valproic acid
2. Gabapentin
74
what drug is used in combination with lithium to tx **refractory bipolar disorder**
Carbamazepine
75
drug interactions with Carbamazepine
* **CYP450 inducer**
* increases toxicity of isoniazid, erythromycin, cimetidine etc
76
unique adverse effect of Carbamazepine
* **steven's johnson syndrome**
* toxic epidermal necrolysis
pharm III exam 1
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