Neuroleptics

Question 1

Alpha-methyltyrosine

Answer 1

Inhibits dopamine synthesis

Question 2

Reserpine

Answer 2

Interferes with vesicular storage of dopamine

Question 3

Bromocriptine

Answer 3

D2 agonist

Overcomes the D2 receptor blockade by neuroleptic D2 antagonist drugs

Clinical treatment for Malignant Neuroleptic Syndrome

Question 4

Diazepam & Dantrolene

Answer 4

Clinical treatment for malignant neuroleptic syndrome

Administered to counteract muscular rigidity of the syndome.

Question 5

Chlorpromazine

Answer 5

D2 receptor antagonist - prototype drug - typical neuroleptic

Treatment for schizophrenia and bipolar disorder

Side Effects: Parkinsonism, Akathisia (uncontrolled restlessness), Dystonia/Dyskinesia (movement dysfunction), Tardive Dyskinesia (involuntary repetitive body movements), Malignant neuroleptic syndrome.
Endocrine effects (hyperprolactinaemia, metabolic syndrome)

Question 6

Fluphenazine

Answer 6

D2 receptor antagonist - typical neuroleptic

Also has action at muscarinic, alpha-1, H1 & 5-HT2a receptors (small action)

Treatment for schizophrenia and bipolar disorder

Side Effects: Parkinsonism, Akathisia (uncontrolled restlessness), Dystonia/Dyskinesia (movement dysfunction), Tardive Dyskinesia (involuntary repetitive body movements), Malignant neuroleptic syndrome.
Endocrine effects (hyperprolactinaemia, metabolic syndrome)

Question 7

Haloperidol

Answer 7

D2 receptor antagonist - typical neuroleptic

Treatment for schizophrenia and bipolar disorder

Side Effects: Parkinsonism, Akathisia (uncontrolled restlessness), Dystonia/Dyskinesia (movement dysfunction), Tardive Dyskinesia (involuntary repetitive body movements), Malignant neuroleptic syndrome.
Endocrine effects (hyperprolactinaemia, metabolic syndrome)

Question 8

Clozapine

Answer 8

Atypical neuroleptic

Order of affinity:-

1. alpha-1 receptor antagonism
2. 5-HT2a receptor antagonism
3. D1 & D2 receptor antagonism (weak affinity)

High risk of seizures, WBC needs monitoring as can induce agranulocytosis (severe and dangerous leukopenia)

Question 9

Risperidone

Answer 9

Atypical neuroleptic

1. 5-HT receptors (highest affinity)
2. D2 receptors

Question 10

Aripiprazole

Answer 10

Atypical neuroleptic

D2 partial agonist
Complete block of 5HT2c and 5HT1a receptors

Less motor side effects than other neuroleptics
Unlikely to cause metabolic syndrome see in typical neuroleptics.