517-518: Psych Drugs 1

Question 1

What is haloperidol? What other drugs are in this class?

Answer 1

Typical antipsychotic; the “-azines” are others in this class including trifuloperazine, fluphenazine, thioridazine, chlorpromazine

Question 2

What is the mechanism of action of typical antipsychotics?

Answer 2

block dopamine D2 receptors (↑ [cAMP])

Question 3

What are typical antipsychotics used for?

Answer 3

schizophrenia (primarily positive symptoms), psychosis, acute mania, and Tourette syndrome

Question 4

What is an example of the extrapyramidal side-effects of typical antipsychotics? How do you treat?

Answer 4

e.g. dyskinesias; treat with benztropine

Question 5

What is an example of the endocrine side effects of typical antipsychotics?

Answer 5

e.g. dopamine receptor antagonism → hyperprolactinemia → galactorrhea

Question 6

What is an example of the muscarinic blocking side effects of typical antipsychotics?

Answer 6

dry mouth, constipation

Question 7

What is an example of the α1 side effects of typical antipsychotics?

Answer 7

hypotension

Question 8

What occurs when antipsychotics interact with histamine receptors?

Answer 8

sedation

Question 9

Do antipsychotics stay in the body for short or long periods of time? Why?

Answer 9

highly lipid soluble and stored in body fat → slow removal

Question 10

Which typical antipsychotics have high potency? Low?

Answer 10

Trifluoperazine, Fluphenazine, and Haloperidol (“Try to Fly High”); Chlorpromazine, Thioridazine (“Cheating Thieves are low”)

Question 11

What kind of side effects are associated with high and low potency typical antipsychotics?

Answer 11

High: neurologic
Low: non-neurologic (anticholinergic, anti histamine, α1 blockade)

Question 12

Categorize the side effects of typical antipsychotics:

Answer 12

Slow removal from body
Extrapyramidal
Endocrine
Blocking of muscarinic, α1, and histamine receptors
Neuroleptic malignant syndrome (NMS)
Tardive dyskinesia

Question 13

What characterizes the neuroleptic malignant syndrome?

Answer 13

FEVER:
Fever (hyperpryrexia)
Encephalopathy
Vitals unstable (autonomic instability)
Enzymes ↑ 
Rigidity of muscles (→ myoglobinuria)

Question 14

How do you treat the neuroleptic malignant syndrome?

Answer 14

Dantrolene, D2 agonists (e.g. bromocriptine)

Question 15

What is tardive dyskinesia?

Answer 15

stereotypic oral-facial movements as a result of long-term antipsychotic use – potentially irreversible

Question 16

What effects do chlorpromazine and thioridazine have on the eyes?

Answer 16

Chlorpromazine = Corneal deposits
Thioridazine = reTinal deposits

Question 17

Which antipsychotic causes NMS and tardive dyskinesia?

Answer 17

Haloperidol

Question 18

What is the evolution of EPS side effects?

Answer 18

• 4 hour acute dystonia (mm. spasm, stiffness, oculogyric crisis)
• 4 day akathisia (restlessness)
• 4 week bradykinesia (parkinsonism)
• 4 month tardive dyskinesia

Question 19

What is akathisia?

Answer 19

restlessness

Question 20

What are the atypical antipsychotic drugs?

Answer 20

“It’s atypical for OLd CLOsets to QUIETly RISPER from A to Z.”

• Olanzapine
• Clozapine
• Quetiapine
• Risperidone
• Aripiprazole
• Ziprasidone

Question 21

What is the mechanism of atypical antipsychotics?

Answer 21

Not completely understood. Varied effects on 5-HT2, dopamine, and α and H1 receptors

Question 22

Clinical use of atypical antipsychotics

Answer 22

1. Schizophrenia - both + and - symptoms
2. Bipolar d/o
3. OCD
4. Anxiety d/o
5. Depression
6. Mania
7. Tourette syndrome

Question 23

What is one benefit of typical vs. atypical antipsychotics?

Answer 23

There are fewer extrapyramidal and anticholinergic side effects in atypicals

Question 24

Which antipsychotics cause significant weight gain?

Answer 24

olanzapine/clozapine

Question 25

Which atypical antipscyhotic is associated with agranulocytosis and seizures?

Answer 25

Clozapine - note that weekly monitoring of WBC levels is required ("must watch clozapine closely")

Question 26

Which antipsychotic causes increase prolactin? What is the effect?

Answer 26

Risperidone - causes: 1. → lactation and gynecomastia 2. → ↓ GnRH, LH, and FSH → irregular menstruation and fertility issues

Question 27

Which antipsychotic may prolong the QT interval?

Answer 27

Ziprasidone

Question 28

What is the mechanism of lithium?

Answer 28

Not established; possibly related to inhibition of phosphoinositol cascade

Question 29

Clinical use for lithium?

Answer 29

Mood stabilizer for BP; blocks relapse and acute manic events. Also SIADH

Question 30

Side effects of lithium?

Answer 30

``` LMNOP: Lithium side effects-- Movement (tremor) Nephrogenic diabetes insipidus hypOthyroidism Pregnancy problems ```

Question 31

Toxicities of lithium?

Answer 31

Tremor, sedation, edema, heart block, hypothyroidism, polyuria (ADH antagonist → nephrogenic DI), teratogenesis, fetal heart defects including Ebstein anomaly and malformation of great vessels.

Question 32

What are some considerations regarding the therapeutic window of lithium?

Answer 32

Narrow therapeutic window → close monitoring of serum levels req'd

Question 33

How do the kidneys handle Li?

Answer 33

most is reabsorbed at the PCT following Na+ reabsorption

Question 34

What is the mechanism of action of buspirone?

Answer 34

Stimulates 5-HT1A receptors

Question 35

Clinical use of buspirone?

Answer 35

GAD -- "I'm always anxious if the bus will be on time, so I take BUSpirONe"

Question 36

What are some benefits of using buspirone over other treatments for anxiety?

Answer 36

Doesn't cause sedation, addiction, or tolerance; does not interact with alcohol (v. benzos and barbs)

Question 37

How long does it take buspirone to take effect?

Answer 37

1-2 wks

Question 38

Which drugs inhibit NE reuptake?

Answer 38

TCAs, SNRIs

Question 39

Which drug promotes NE release from the presynaptic terminal?

Answer 39

buspirone

Question 40

Which drug inhibits the α2 receptor on the noradrenergic cell? Effect?

Answer 40

mirtazapine; ↑ release of NE (b/c α2 tonically inhibits NE release into synapse)

Question 41

Which drugs inhibit 5-HT reuptake?

Answer 41

TCAs, SSRIs, SNRIs, trazodone

Question 42

Which two pathways do MAO inhibitors work on?

Answer 42

noradrenergic (NE), and serotonergic (5-HT)