Pcol 1 Test 2

Front 1

Two broad categories of antipsychotic drugs.

Back 1

Typical and Atypical

Front 2

1st Generation Antipsychotics are called:

Back 2

Typical Antipsychotics

Front 3

2nd Generation Antipsychotics are called:

Back 3

Atypical Antipsychotics

Front 4

3rd Generation Antipsychotics are called:

Back 4

Dopamine Partial Agonists

Front 5

What is the one major 3rd Gen. Antipsychotic?

Back 5

Aripiprazole

Front 6

A/typical antipsychotics block what receptor?
What other receptor does atypical drugs block?

Back 6

- D2 Receptors
- 5-HT2 Receptors

Front 7

What are the subtypes of Dopamine receptors?
How are these further divided?

Back 7

- D1-D5
- D1 like (D1, D5)
- D2 like (D2-D4)

Front 8

What is the difference between an antagonist and an inverse agonist?

Back 8

Antagonists have no activity but have affinity to sites. Inverse agonists have affinity site, but they also produce the opposite effect of an agonist.

Front 9

What symptoms do 1st Generation Antipsychotics treat best?

Back 9

Positive symptoms

Front 10

What symptoms do 2nd Generation Antipsychotics treat best?

Back 10

Negative symptoms

Front 11

What symptoms do 3rd Generation Antipsychotics treat best?

Back 11

Extrapyrimidal symptoms due to the 5-HT2A receptors.

Front 12

What is the order of binding for Typical (1st Gen) Antipsychotics?

Back 12

D2~D1>a1~5-HT2

Front 13

What is the order of binding for Atypical (2nd Gen) Antipsychotics?

Back 13

D2~5-HT2>>D1>a1

Front 14

What is the order of binding for 3rd Generation antipsychotics?

Back 14

Partial agonism of D2,
5-HT1a
There is ANTAGONISM of
5-HT2a

Front 15

Phenothiazine Derivatives:
What is the name of the standout drug?

Back 15

Chlorpromazine

Front 16

Phenothiazine Derivatives:
What kind of receptors do they act on?

Back 16

They DO NOT differentiate between D1 or D2 receptors.

Front 17

Phenothiazine Derivatives:
What is the specific structure that deals with the receptor?

Back 17

The 3* Amine

Front 18

Phenothiazine Derivatives:
Hydro or Lipophilic?

Back 18

They are VERY lipophilic

Front 19

Phenothiazine Derivatives:
What is the significance of bioisosteres in this class?

Back 19

Although bioisosteres can occur, activity is still retained.

Front 20

Phenothiazine Derivatives:
The phenyl rings are lipo/hydrophilic.

Back 20

Lipophilic

Front 21

Phenothiazine Derivatives:
What effect do the benzene rings do to the acidity of the N?

Back 21

They are electron withdrawing so it causes the N to become weakly BASIC.

Front 22

Phenothiazine Derivatives:
True/False, The N can be cationized at physiological pH.

Back 22

False. It is not cationized at physiological pH.

Front 23

Phenothiazine Derivatives:
What effect does the 3* amine have on the basicity of the compound?

Back 23

The 3* amine also gives strong basicity to the compound.

Front 24

Phenothiazine Derivatives:
What must you do to the compound to make it suitable for oral suspensions?

Back 24

You must make the compound more hydrophilic.

Front 25

Phenothiazine Derivatives:
What must you do in order to decrease the hydrophilicity make it long-acting? Describe the specific mechanism.

Back 25

You must make the compound more lipophilic by esterifying the --OH group on the 3* amine chain. (Prodrug)

Front 26

Phenothiazine Derivatives:
Why is the 3-C spacer very important for activity?

Back 26

This allows free rotation of the bonds around the N.

Front 27

Phenothiazine Derivatives:
How do you lock the free rotation?

Back 27

A bioisostere should be formed (Double-bond will form).

Front 28

Phenothiazine Derivatives:
What conformation has more activity?

Back 28

The CIS conformation does.

Front 29

Schizophrenia:
True/False - It is an idiopathic psychosis. What does that mean?

Back 29

True. Schizophrenia is idiopathic. That means that the cause is not known.

Front 30

Schizophrenia:
What are the two broad categories of symptoms?

Back 30

Positive/Negative symptoms

Front 31

Schizophrenia:
True/False - Both positive and negative symptoms of Schizophrenia can be found in unaffected patients.

Back 31

False. Only negative symptoms are found in un/affected patients.

Front 32

Schizophrenia:
Describe some of the positive symptoms:

Back 32

Hallucinations (Auditory), Delusions, Grandiosity, Catatonia, Paranoia.

Front 33

Schizophrenia:
Describe some of the negative symptoms:

Back 33

Disordered (Illogical) Thinking, Withdrawal, Depersonalization, Emotional Changes.

Front 34

Schizophrenia:
What is the age range of onset?

Back 34

Late adolescence to young adulthood.

Front 35

Schizophrenia:
What are possible sources of this disorder?

Back 35

It can be genetic, or environmental/experiential contribution.

Front 36

Schizophrenia:
True/False - If a twin has this disorder, only 10% chance that other twin will have disorder.

Back 36

False. The chance is around 50%.

Front 37

Schizophrenia:
Although the disease is chronic, what effect does treatment have on patients?

Back 37

1/3 of patients will improve w/ medication.
1/3 of patients will have periodic relapses.
1/3 of patients will worsen.

Front 38

Schizophrenia: What receptor must be blocked in order to treat the disease?

Back 38

The DA receptor.

Front 39

Supporting The dopamine theory of Schizophrenia:
What is the significance of blocking DA receptors?

Back 39

Psychotic symptoms are reduced, especially positive ones.

Front 40

Supporting The dopamine theory of Schizophrenia:
What is the significance of Amphetamine/Cocaine?

Back 40

These two substances will also produce similar symptoms to schizophrenia.

Front 41

Supporting The dopamine theory of Schizophrenia:
What happens to the D2 receptors of untreated schizophrenic patients?

Back 41

There is an increase in the number of receptors.

Front 42

Supporting The dopamine theory of Schizophrenia:
How are the blockade of D2 receptors and anti-psychotic durg potency related?

Back 42

There is a correlation between those two things.

Front 43

Against the dopamine theory of Schizophrenia: How are the DA levels, DA cell activity evidence agianst the theory.

Back 43

There is no evidence showing increased levels of DA cell activity or DA levels in the bain.

Front 44

Against the dopamine theory of Schizophrenia: What is the wrong with the correlation between receptor blockade and antipsychotic effect? On what dose should effects appear to be a good antipsychotic drug?

Back 44

Correlation also does not prove cause. The antipsychotic effect takes too long to appear. (Up to weeks). 1st dose is the standard.

Front 45

Schizophrenia: What receptor do all current drugs act on? What are the difficulties with this, and what are the side effects?

Back 45

They all act on blocking DA receptors. However, it is hard to selectively block the receptors only in the limbic area and this causes EPS and endocrine s/e.

Front 46

What are the 3 antipsychotic drug classes?

Back 46

Phenothiazine derivatives, Thioxanthene derivatives and Butyrophenone derivatives.

Front 47

What are the drugs in the phenothiazine derivative class?

Back 47

Chlorpromazine (Prototype)
Thioridazine
Trifluoperazine
Perphenazine
Fluphenazine

Front 48

What are the drugs in the thioxanthene derivative class?

Back 48

Thioxanthene
Chlorprothixene

Front 49

What are the drugs in the butyrophenone derivative class?

Back 49

Haloperidol
Droperidol
Spiroperidol

Front 50

How much more effective is Haloperidol over Chlorpromazine?

Back 50

100x more.

Front 51

What are the drugs in the atypical antipsychotic drug class?

Back 51

Pimozide
Molindone
Clozapine
Risperidone
Olanzapine
Loxapine
Quetiapine
Ziprasidone
Aripiprazole

Front 52

Instead of D2 receptors, what receptors are atypical antipsychotics better at blocking?

Back 52

They are better at blocking
5-HT2 receptors.

Front 53

Antipsychotic Drugs: What are some CNS s/e?

Back 53

Sedation, Antianxiety, NEUROLEPTIC Syndrome: (Only common with older drugs) = No rapid responses, impaired vigilance.

Front 54

Antipsychotic Drugs: What are some endocrine s/e?

Back 54

Increase prolactin secretion
Up F, Down M libido
Increase appetite/weight gain
Type 2 Diabetes
Hypothermic effect

Front 55

What happens when prolactin secretion is increased?

Back 55

Breast enlargement in M
Ameno/Galactorrhea in F

Front 56

What antipsychotic drugs will cause prolactin secretion?

Back 56

All typical antipsychotics and risperidone. The atypicals have minimal effects on secretion.

Front 57

Antipsychotic Drugs: What are CRTZ and Autonomic side effects?

Back 57

Anti-emetic
Muscarinic blockade (Blurred vision, dry mouth, constipation, difficulty urinating)
A-receptor blockade (Orthostatic hypertension, reflex tachycardia, impotence)

Front 58

Antipsychotic Drugs: What are the CVS s/e:

Back 58

Hypotension, ECG changes, Cardiotoxicity

Front 59

Antipsychotic Drugs: What are some blood disorders?

Back 59

Leukopenia (Decreased WBC count)
Eisinophilia (Increased certain elements)

Front 60

What is a major blood disorder that Clozapine can cause?

Back 60

Marrow suppression and Agranulocytosis. Symptoms would appear w/in the first few weeks of use.

Front 61

Antipsychotic Drugs: What are some EPS? Why do these occur?

Back 61

Parkinsonian (It is NOT Parkinson's disease), Dystonic Reactions (Seizure-like), Akathesia, Neuroleptic Malignant Syndrome, Tardive Dyskinesia.

Front 62

How can you treat tardive dyskinesia?

Back 62

You can't. The only way is to avoid using strong D2 blockers or to only use the lowest effective dose as possible.

Front 63

What is the mechanism of tardive dyskinesia?

Back 63

By blocking the DA receptors, this causes an increase in the number of D2 receptors in the striatum.

Front 64

Antipsychotic Drugs: What are some skin s/e?

Back 64

Hypersensitivity
Contact Dermatitis
Photosensitivity (Sunburn-like)
Abnormal skin colors (Only with long-term use)

Front 65

Antipsychotic Drugs: Why must care be taken when dealing with epileptics?

Back 65

This is because the sizure threshold is lowered.

Front 66

Antipsychotic Drugs: What are some possible drug interactions?

Back 66

CNS Depressants, Sedatives, Alcohol, Opiates, Benzodiazepines.

Front 67

Antipsychotic Drugs: Clozapine can suppress or not cause what major side effects?

Back 67

EPS and Tardive Dyskinesia