General for typical/atypical antipsychotics

Question 1

Describe neuroleptic malignant syndrome

Answer 1

Hyperthermia & autonomic dysfx –> decreased reflexes & lead pipe rigidity

Question 2

What is neuroleptic malignant syndrome due to?

Answer 2

Dopamine block (antipsychotics).. Especially Haloperidol & Chlorpromazine

Question 3

Tx of neuroleptic malignant syndrome?

Answer 3

Bromocriptine (DA agonist), Dantroline (muscle relaxer), Lorazepam

Question 4

Effects of antipsychotics on organ systems.. here we go. CNS?

Answer 4

The CNS does not adapt to DA blockade –> decreased threshold for seizures

Question 5

Basal ganglia?

Answer 5

Decreased dopamine in basal ganglia is basis for EPS; this does adapt over time w/ increased dopamine synthesis & firing

Question 6

Limbic system?

Answer 6

Therapeutic effects occur here

Question 7

Hypothalamus?

Answer 7

Increased prolactin secretion; avoid in pts w breast cancer!

• Prolactin secretion worst w/ all the typicals & Risperidone
• No prolactin secretion w/ Quetiapine & Aripiprazole
• No antipsychotics w/ breast cancer!

Question 8

CTZ?

Answer 8

N/V are activated by dopamine

Question 9

Renal?

Answer 9

Chlorpromazine = antidiuretic

Question 10

Hepatic?

Answer 10

Maybe toxic in liver dz

Question 11

Endocrine?

Answer 11

• Chlorpromazine impairs glucose tolerance & decrease insulin release
• Clozapine, Risperidone, Ariprizole, Ziprasidone, Olanzepine, Quetiapine –> increased risk for DM 2

Question 12

CVD?

Answer 12

Chlorpromazine & Thioridazine block alpha adrenergic receptors –> orthostatic hypoTN

Question 13

What is an ADE 4 hours after antipsychotics?

Answer 13

Acute dystonia: stiff, distorted areas & oculogyeric crisis

-Tx w/ anticholinergics & anti-parkinson (Benztropine)

Question 14

ADE after 4 days?

Answer 14

Akathesia: “restless legs”

-Tx is to decrease doseage

Question 15

ADE after 4 weeks?

Answer 15

Bradykinesia (Parkinsonism)
-Tx w/ benztropine or amantadine but NOT L-Dopa/Bromocriptine cuz a high dopamine is what caused the psychosis to begin with

Question 16

What is perioral tremor?

Answer 16

aka “rabbit syndrome”; mimics movements

-Tx w/ anticholinergic

Question 17

ADE after 4 months?

Answer 17

Tardive dyskinesia- oral/facial movements; assc w/ long term antipsychotic use; usually irreversible

Question 18

What antipsychotic causes jaundice?

Answer 18

Chlorpromazine

Question 19

Blood dyscrasias (agranulocytosis)?

Answer 19

Clozapine

Question 20

Skin reactions?

Answer 20

Phenothiazines (Chlorpromazine, Fluphenazine, Perphenazine).. But mostly Chlorpromazine

Question 21

Weight gain?

Answer 21

Clozapine & Olanzapine

-In children/adolescents the atypicals –> weight gain

Question 22

Metabolic syndrome?

Answer 22

Olanzapine

Question 23

Lipid soluble?

Answer 23

Yes

Question 24

Highly protein bound?

Answer 24

Yes

Question 25

Cross placenta? Breast milks?

Answer 25

Yes

Question 26

How are the antipsychotics metabolized?

Answer 26

They are oxidized via CYP2D6/3A4 to inactive products (except chlorpromazine, phenothiazines, respiradone, ehydroaripirazonle metabolites are not inactive)

Question 27

DDIs?

Answer 27

They inhibit CYP2D6 –> increase TCA/SSRI

Question 28

What antipsychotics are long acting “depot” drugs that you give to non-compliant pts or to patients with low oral bioavailability?

Answer 28

1. Prolixin decanoate
2. Haldol decanoate
3. Resperidal consta

Question 29

MOA of the long acting antipsychotics?

Answer 29

Combine anti-psychotic w/ decanoic acid (fatty acid) –> esterifies alcohol group –> produces lipophilic compound
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