Antipsychotics

Question 1

Neuroleptic dug MOA?

Answer 1

Blockade of dopamine receptors in the brain.

Atypical neuroleptics also act as antagonists or partial antagonists to serotonin receptors.

Question 2

The chief antipsychotic effects of neuroleptic drugs appear related to the dopamine blockade at which receptor site?

Answer 2

D2 receptors

Question 3

Psychotic experiences have been linked to excess release of __________ in the ___________ pathway?

Answer 3

Psychotic experiences have been linked to excess release of dopamine in the mesolimbic pathway?

Question 4

Common SE of neuroleptic drugs

Answer 4

Tremors/Parkinsonian effects
Tardive dyskinesia
Blurred vision, dry mouth, constipation
Urinary retention
Increased prolactin release

Question 5

What is tardive dyskinesia?

Answer 5

Facial grimacing and inappropriate posturing of the tongue, neck, trunk and limbs

Tardive = continues on or first appears after drugs are no longer being taken.

Question 6

What is neuroleptic malignant syndrome?

Answer 6

Additional SE that rarely occurs. Characterized by catatonia, fluctuating BP, dysarthria and fever.

Question 7

What is the protocol when a case of neuroleptic malignant syndrome comes on?

Answer 7

Immediately discontinue drug and tx with dopamine agonist like BROMOCRIPTINE.

Question 8

Neuroleptic drugs can also be helpful in tx this condition due to the fact that they block D2 receptors in the chemoreceptor trigger zone of the medulla?

Answer 8

Severe nausea

Neuroleptics are anti-emetic

Question 9

Chlorpromazine/Thorazine
Class:
Ind:
MOA:

Answer 9

Chlorpromazine/Thorazine
Class: Neuroleptic
Ind: Psychosis, mania, schizophrenia, N/V, intractable hiccoughs
MOA: D2 dopaminergic receptor site blockade.

Add’l MOA: alpha-adrenergic blockade and H1 blockade

Question 10

What hormone commonly has an increased release as a result of the dopamine blockade?

Answer 10

Prolactin

SE: galactorrhea and amenorrhea in women and infertility in both sexes

Question 11

Prochlorperazine/Compazine
Class:
Ind:
MOA:

Answer 11

Prochlorperazine/Compazine
Class: Typical neuroleptic
Ind: Psychosis, vertigo, N/V associated with migraine HA
MOA: Primarily H1-histamine receptor antagonist as well as alpha-adrenergic receptor antagonist and D2 dopaminergic receptor antagonist

Question 12

Prochlorperazine/Compazine
Char:
SE:

Answer 12

Prochlorperazine/Compazine
Char: Less orthostatic hypotension, fewer extrapyramidal signs, better anti-emetic than other neuroleptics
SE: Lowers seizure threshold

Question 13

Haloperidol/Haldol
Class:
Ind:
MOA:

Answer 13

Haloperidol/Haldol
Class: Typical neuroleptic
Ind: Psychosis, tourette’s, Huntington’s dz, ACUTE AGITATED BEHAVIOR
MOA: D2 dopaminergic receptor site blockade

Question 14

Haloperidol/Haldol
Char:
SE:

Answer 14

Haloperidol/Haldol
Char: Careful administration to reduce excessive sedation and tardive dyskinesia
SE: Parkinsonian-like sx, extrapyramidal effects, tremor, NEUROLEPTIC MALIGNANT SYNDROME

Question 15

Clozapine/Clozaril
Class:
Ind:
MOA:
Char:

Answer 15

Clozapine/Clozaril
Class: Atypical neuroleptic
Ind: Schizophrenia
MOA: Receptor site blockade at D2 and 5-HT2 (serotonin) receptors
Char: PO, rapid absorption and extensive metabolism

Question 16

Clozapine/Clozaril

SE

Answer 16

Diminished extrapyramidal SE comparatively.

AGRANULOCYTOSIS in 1-2% of pt. (discontinue use of granulocyte count is

Question 17

Respiradone/Risperdal
Class:
Ind:
MOA:
Char:

Answer 17

Respiradone/Risperdal
Class: Atypical neuroleptic
Ind: Psychosis
MOA: unknown….presumed dopamine and serotonin receptor blockade
Char: Metabolized via P450 enzymes (dose reduced in pt with liver dysfunction)

Question 18

Respiradone/Risperdal

SE (in addition to common)

Answer 18

Weight gain
Hyperglycemia
DM
Increased risk for stroke

Question 19

Olanzapine/Zyprexa
Class:
Ind:
MOA:
Char:

Answer 19

Olanzapine/Zyprexa
Class: Atypical neuroleptic
Ind: Schizophrenia
MOA: Receptor site blockade (D2 and 5-HT2)
Char: PO, rapid absorption and metabolism

Question 20

Olanzapine/Zyprexa

SE

Answer 20

Weight gain
Hyperglycemia
DM
Increased risk for stroke

Question 21

Which to atypical neuroleptics have SE of weight gain, hyperglycemia, DM and increased risk for stroke?

Answer 21

Respiradone/Risperdal

Olanzapine/Zyprexa

Question 22

What is used to prophylactically treat manic episodes of bipolar disorder?

Answer 22

Lithium salts

Question 23

What is a major char of Lithium carbonate/Eskalith?

Answer 23

Very small therapeutic index, cleared by the kidneys

Question 24

Major SE of Lithium carbonate/Eskalith?

Answer 24

MC renal effect: impaired concentration capacity due to reduced renal response to ADH.

Nephrogenic Diabetes Insipidus (20% w/chronic tx)

Hypothyroidism (5-35% w/chronic tx)