Antipsychotics

Question 1

What are the 5 most prescribed antipsychotic drugs in the U.K.?

Answer 1

Atypical:

1st: Quetiapine
2nd: Olanzapine
3rd: Risperidone
4th: Aripiprazole

Typical:

5th: Chlorpromazine

Question 2

What are the two pathways behind the theory of schizophrenia?

Answer 2

1) Mesocortical Pathway:
- Dopamine underactive
- D1 receptors predominate
- Negative symptoms

2) Mesolithic Pathway:
- Dopamine overactive
- D2 receptors predominate
- Positive symptoms

Question 3

Drugs that release ____ or activate associated pathways induce psychosis- like effect. E.g. L-DOPA, amphetamines, bromocriptine.

Answer 3

Dopamine (and schizophrenic patients have increased DA release)

Question 4

Dopamine (agonists/ antagonists) cause psychosis?

Dopamine (agonists/ antagonists) cause anti-psychotic effects?

Answer 4

Agonist

Antagonist

Question 5

MOA of anti-psychotic drugs:

Answer 5

Bloakade of dopamine and/ or 5HT(2) receptors

Question 6

S/E of dopamine blockade.

Answer 6

1) Dyskinesia
- acute EPS: extrapyramidal symptoms e.g. acute dystonia
- chronic EPS e.g. Tardrive dyskinesias

2) Dysphoria
3) Endocrine dysfunction (temp/ increase prolactin, increase eating disorder)

Question 7

S/E of muscarinic blockade.

Answer 7

Tachycardia and decrease seizure threshold

Question 8

S/E of alpha blockade.

Answer 8

Hypotension

Question 9

Antipsychotic drugs not only act as ______, but also modify ________ function.

Answer 9

DA antagonists

Serotonin

Question 10

Name two drugs that act primarily as D1 receptor antagonists.

Answer 10

Olanzapine and Zuclopenthixol

Question 11

Name two drugs that act primarily as D2 receptor antagonists (Gi GPCR).

Answer 11

Olanzapine
Risperidone 
Aripiprazole 
Zuclopenthixol
Haloperidol 

(Either two)

Question 12

Name two drugs that act primarily as Alpha-1 (alpha- adreniceptors 1: Gq GPCRs) receptor antagonists.

Answer 12

Quetiapine
Chlorpromazine
Zuclopenthixol
Clozapine

(either two)

Question 13

Name two drugs that act primarily as H1 (histamine 1- Gq GPCRs) receptor antagonists.

Answer 13

Quetiapine
Chlorpromazine
Clozapine

(either two)

Question 14

Name two drugs that act primarily as 5-HT (especially 5-HT2A) receptor antagonists.

Answer 14

Olanzapine
Risperidone 
Aripiprazole 
Chlorpromazine
Zuclopenthixol
Clozapine

(Either two)

Question 15

Name two drugs that act primarily as muscarinic AChRs (Gq/GI GPCRs) receptor antagonists.

Answer 15

Olanzapine
Chlorpromazine
Clozapine

(either two)

Question 16

There are (a lot/ only a few) antipsychotic drugs in the U.K..

Answer 16

A lot

Question 17

Common sides effects of antipsychotics.

Answer 17

1) EPS (extrapyramidal symptoms) (D2/D1)
- acute EPS: e.g. acute dystonia
- chronic EPS e.g. Tardrive dyskinesias

2) Endocrine dysfunction (temp/ increase prolactin, increase eating disorder/ breast swelling, pain lactation) ( D2/ D1)
3) sedation (H1 histamine receptor)
4) Weight gain (H1, 5-HT, mAChR)
5) Hypotension (alpha-adrenoceptors)
6) Anticholinergic effects e.g. Dry mouth blurred vision. (mAChR)
7) Autonomic S/E: constipation, dry mouth and hypotension.
8) other S/E: drowsiness, tachycardia

Question 18

Examples of first generation/ typical antipsychotics.

Answer 18

• Chlorpromazine (phenothiazine class)
• Haloperidol (Butyrophenone class)
• Zuvlopenthixol (Thioxabthene class)

Question 19

First (typical) / second (atypical) generation antipsychotics are less likely to cause EPS. And give some examples.

Among all, ______ is highly recommended with treatment resistance.

Answer 19

Second generation/ atypical.

Examples: clozapine, Quetiapine, Olanzapine, Risperidone, Aripiprazole, Sulpiride.

Clozapine is highly recommended with treatment resistance.

Question 20

What is the two most prescribed antipsychotics in the UK?

Answer 20

1st: Quetiapine
2nd: Olanzapine

Question 21

What is atypical antipsychotics?

Answer 21

Antipsychotics that are free or relatively free of EPSs (extrapyramidal S/E). These may reduce negative symptoms of schizophrenia.

Question 22

D1 stimulate ______ (enzyme).

Answer 22

Adenylyl cyclase

Question 23

Blockage of D2 in basal ganglia usually results in ___.

Answer 23

EPS

Question 24

Deep IM antipsychotic injection is act as ___________ injections in community to decrease risk of patients forgetting daily doses.

Answer 24

Long- action depot injections.

Question 25

Endocrine effect of increasing prolactin production after D2 receptor blockade.

Answer 25

Gynaecomastia, galactlrrhoea, menstrual irregularities, impotence, weight gain.