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CNS > Schizophrenia Med Chem > Flashcards

Schizophrenia Med Chem Flashcards

1
Q

Regarding the metabolism of the Typical Antipsychotic Trifluoperazine (Stelazine) what types of metabolisms can occur at the circled points? (select all)

A. Hydroxylation

B. Methylation

C. Oxidation

D. Esterification

E. Demethylation

A

A. Hydroxylation

C. Oxidation

E. Demethylation

The top circled group with the nitrogen can undergo demethylation

The lower left benzyl group can undergo hydroxylation

The lower sulfur group can undergo oxidation and form a sulfoxide

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2
Q

The medications Trifluoperazine (Stelazine) has a K.I value of 1.1 and Chlorpromazine (Thorazine) has a K.I value of 2.0. What does this mean in terms of D2 receptor antagonism and affinity?

A. Stelazine has higher D2 receptor affinity but Chlorpromazine has higher incidence of EPS.

B. Chlorpromazine has higher D2 receptor affinity but Stelazine has higher incidence of EPS

C. Both medications have the same D2 receptor affinity but Trifluoperazine has a higher incidence of EPS

D. Stelazine has higher D2 receptor affinity and a higher incidence of of EPS.

A

D. Stelazine has higher D2 receptor affinity and a higher incidence of of EPS.

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3
Q

The following medications Fluphenazine and Perphenazine feature (n) groups that were added on to the medications and give them an enanthate and decanoate formulation. What is the advantage of this? (Select All)

A. Stronger D2 antagonism

B. Makes them longer-acting antipsychotics

C. Makes them short-acting antipsychotics for acute emergencies

D. Possibly improves patient compliance with less frequent dosing

E. Allows the medication to form numerous active metabolites that each have a longer half-life

A

B. Makes them longer acting antipsychotics

D. Possibly improves patient compliance with less frequent dosing

The n groups are carbon chains that can be 5 carbons long (enanthate) or 8 carbons long (decanoate) and this contributes to longer durations of action.

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4
Q

The Typical Antipsychotic Haloperidol (Haldol) contains a ___ functional group.

A. Decanoate

B. Phenothiazine

C. Fluorobutyrophenone

D. Enanthate

A

C. Fluorobutyrophenone

Fluoro-Fluorine

Butyro-Butyl (4 carbons)

Phenone- Phenyl group + Ketone

FluoroButyroPhenone

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5
Q

In the FGA Chlorpromazine what is the name of the functional group that circled?

A. Phenothiazine

B. Benzylthiazole

C. Dibenzylheptene

D. Dibenzylchloranthate

A

A. Phenothiazine

Pheno-Phenyl groups (2)

Thi- Thiol=sulfur

Azine- Azole=nitrogen

PhenoThiAzine

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6
Q

Haldol has a K.I value of 1.0. As a result it will have ___ D2 receptor binidng affinty and ___ EPS side effects.

A. Low, High

B. High, Low

C. Low, Low

D. High, High

A

D. High, High

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7
Q

Haldol forms 3 different metabolites. The one highlighted in the picture provided is known as a(n) ___.

A. Pyrazine

B. Tertiary Pyradine

C. Quaternary Pyridinium

D. Dibenzylnitrate

A

C. Quaternary Pyridinium

The nitrogen has a charge now and is known as a quaternay structure.

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8
Q

What is the issue with the Quaternary pyridinium metabolite that is generated from Haloperidol (Haldol)?

A. Hepatotoxic to liver cells

B. Neurotoxic to dopaminergic cells

C. Nephrotoxic to kidney cells

D. Cardiotoxic to heart cells

A

B. Neurotoxic to dopaminergic cells

With constant exposer it can cause Tardive Dyskinesia

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9
Q

Which of the following statments is true regarding Droperidol (Dridol, Inapsine)?

A. Ultra-Long acting typical antipsychotic

B. Intermediate acting antipsychotic

C. Short-Acting Antipsychotic

D. Virtually no DDIs

A

C. Short-acting Antipsychotic

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10
Q

The typical antipsychotic Pimozide (Orap) is known as a ___ analog.

A. Di-aryl

B. Di-benzyl

C. Di-propyl

D. Di-fluoro

A

A. Di-aryl

It contains two phenyl groups that are also known as “Aromatic” so that is why it is called Di-Aryl

It is also one of the LAIs since it stays in the brain longer

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11
Q

In the general SAR for typical antipsychotics what can the “W” group consist of? (Select All)

A. F

B. Cl

C. CH3

D. OCH3

A

A. F

D. OCH3 (methoxy)

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12
Q

In the general SAR for typical antipsychotics what is true regarding the “X” group?

A. Needs to be an Ether linkage (C-O-C)

B. Must be Ester Linkage

C. Must be a carbonyl group (C=O)

D. Must be an Amide

A

C. Must be a carbonyl group (C=O)

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13
Q

In the SAR for typical antipsychotics how long does the carbon spacer have to be?

A. 1 Carbon

B. 2 Carbons

C. 3 Carbons

D. 4 Carbons

A

C. 3 Carbons

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14
Q

In the SAR for typical antipsychotics, the Ar2 group is preferrably___.

A. Heterocyclic

B. Aromatic

C. A 7 membered ring

D. An 8 membered ring

A

A. Heterocyclic

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15
Q

In the SAR of typical antipsychotics the “Y” group can consist of: (Select All)

A. Aromatic group

B. H group

C. OH group

D. Cl group

A

B. H group

C. OH group

look at slide 17 to see the green structure substitutions

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16
Q

When looking at the metabolism of Clozapine, the top metabolite is a(n) ___ metabolite and the bottom metabolite is a(n) ___ metabolite.

A. N-Desmethyl, N-Oxide

B. N-Oxide, N-Desmethyl

C. N-Oxide, N-Despropyl

D. N-Despropyl, N-Oxide

A

B. N-Oxide, N-Desmethyl

17
Q

If a patient began smoking while on this medication what would you expect to see?

A. Decrease in DMCZ metabolites

B. Increase in DMCZ metabolites

C. Increase in CZNO metabolites

D. No change in metabolite formaiton

A

B. Increase in DMCZ metabolites

The reason for this is because smoke acts as a CYP3A4 and CYP1A2 inducer and will increase the enzyme activity

18
Q

When taking Clozapine why do we instruct patients to reduce their caffeine intake?

A. Caffeine irreversibly inhibits CYP1A2 and 3A4

B. Caffeine competes with Clozapine for CYP1A2 and 3A4 metabolism

C. Caffeine in a PgP inhibitor and can cause potential toxicities of Clozapine

D. Caffeine can chelate with Clozapine and prevent the medication from passing the gut wall.

A
19
Q

What is the name of the core structure of Clozapine (Clozaril)?

A. Dihexylazepine

B. Diheptylazepine

C. Benzazepine

D. Phenothiazine

A

C. Benzazepine

Benz-Benzyl groups

Azepine- nitrogen groups

BenzAzepine

20
Q

What type of reaction is occuring here in the metabolism of Olanzapine?

A. O-Sulfation

B. O-Glucuronidation

C. N-Glucuronidation

D. N-Sulfation

A

C. N-Glucuronidation

21
Q

What metabolisms can Olanzapine undergo? (Select All)

A. N-Methylation

B. N-Demethylation

C. N-Sulfation

D. N-Oxidation

E. N-glucuronidation

A

B. N-Demethylation

D. N-Oxidation

E. N-Glucuronidation

N-Demethylation can occur at the top nitrogen group circled

N-Oxidation also occurs at the top nitrogen group

N-Glucuronidaiton occurs at the bottom Nitrogen group in the blue structure.

22
Q

What is the name of the new core group in Olanzepine?

A. Benzazepine

B. Thienobenzodiazepine

C. Phenothiazine

D. Nitrothioheptene

A

CNS (8 decks)

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