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Phar 752 > Antipsychotics > Flashcards

Antipsychotics Flashcards

1
Q

Chlorpromazine metabolism

A

3A4 to CPZ Sulfoxide (inactive)
2D6 to Nor1-CPZ (weakly active)
Multiple steps to CPZ propionic acid (inactive)
2D6(major)/1A2 to 7-HydroxyCPZ (weakly active)

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2
Q

Fluphenazine decanoate Brand, ROA, Duration

A

N/A
Depot injection.
3-4 weeks.

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3
Q

Side Effects common to AD’s and corresponding receptor targets:

A

Antimuscarinic - M1
Sedative - H1
Hypotensive - alpha-1

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4
Q

Thioridazine metabolism

A

2D6 to Sulfoxide metabolite (active)

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5
Q

Clozapine metabolism*

A

1A2(major)/3A4 to N-desmethyl metabolite (active)

  • Cigarette smoking induces 1A2
  • 3A4 to Reactive Nitrenium Ion
  • Can either react with GSH, or protein nucleophiles, which leads to toxicities.
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6
Q

Olanzapine metabolism

A

1A2 to N-desmethyl metabolite
GSH to 10-N-glucuronide metabolite
(Both inactive?)

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7
Q

Olanzapine pamoate Brand, ROA, Duration

A

Zyprexa Relprevv
IM injection
2-4 weeks

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8
Q

Loxapine metabolism

A

3A4 N-demethylation to Amoxapine (active)

  • Blocks NE reuptake: Antidepressant mechanism.
  • Separate Antidepressant drug.
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9
Q

Quetiapine metabolism

A

Major: 3A4 to Sulfoxide metabolite.
Minor: 3A4 to N-desalkylquetiapine (active).
- Different pharmacological profile
- Fairly potent as M1-antagonist

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10
Q

Asenapine metabolism

A

Major: Glucuronidation at tertiary amine.
Minor: 1A2 to N-desmethyl metabolite.
(Both inactive)

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11
Q

Haloperidol metabolism*

A 
Major routes:
- 3A4/2D6 N-dealkylation
- Reduction of the ketone... by?
*Minor route; three steps:
1 - 3A4 (oxidation?) to positive N-species
2 - Dehydration (possibly by 3A4)
3 - Oxidation (by?)
Left with "HPP+"
- Like MPP+
- Potential neurotoxic metabolite
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12
Q

Haldol decanoate Brand, ROA, Duration

A

Haldol decanoate
Depot injections
4weeks

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13
Q

Risperidone metabolism

A

2D6 to +/=-9-hydroxyrisperidone or “Paliperidone”

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14
Q

Paliperidone metabolism

A

60% excreted unchanged.

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15
Q

Paliperidone palmitate Brand, ROA, Duration

A

Invega Sustenna
Depot Injections
N/A

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16
Q

Iloperidone metabolism

A

Reuction of ketone by? (active)
2D6 hydroxylation (at terminal methyl) (active)
3A4 O-demethylation (inactive)

17
Q

Ziprasidone metabolism

A

1/3 metabolized by P450’s:
- 3A4major/1A2 to sulfoxide/sulfone/N-dealkylation
- Inactive
2/3 metabolized by another route
- 1: Aldehyde oxidase mediates a reduction
- 2: S-methylation by?
- Inactive
Cimetidine should cause an interaction, but it doesn’t for some reason.

18
Q

Aripiprazole metabolism

A

2D6/3A4 to Dehydroaripiprazole (active)

- less potent

19
Q

Aripiprazole Lauoxil Brand, ROA, Duration, AND Metabolism

A

Aristada
IM injection
4-6 weeks
Esterase cleaves ester, product undergoes spontaneous ( ) to form active Aripiprazole.

20
Q

Lurasidone metabolism

A

Major: 3A4 to sulfoxide/sulfone metabolites (inactive)
Hydroxylation (active) - contributes significantly
N-dealkylation (inactive)

21
Q

Brexpiprazole metabolism

A

2D6/3A4…. (inactive)

22
Q

Cariprazine metabolism

A

3A4major/2D6 to Desmethyl/Didesmethyl metabolites

  • Both active
  • Equipotent
  • Contribute significantly
23
Q

Pimvanserin metabolism

A

3A4 to N-desmethyl metabolite (active)

24
Q

What is Adasuve

A

Loxapine as an inhalation powder.

25
Q

Clozapine Characteristics

A 
Advantages:
- Uniquely effective
- No reported EPS
Toxicities: Make it a 3rd line agent:
- Leukopenia to agranulocytosis (1.3% patients)
- Myocarditis
- Cardiovascular collapse
Decreases seizure threshold
Typical SE's as well: Sedation, antimuscarinic effects (notably constipation), etc.
26
Q

Neutropenia definition

A

Neutrophil count under 1500cells/uL in whites

under 1200 in African/Middle eastern

27
Q

Leukopenia

A

WBC under 4000cells/uL

28
Q

FGA and SGA notable for Neutropenia

A

Haloperidol, Olanzapine, Quetiapine, Risperidone

29
Q

Olanzapine characteristics

A

Similar to Clozapine, but lacks toxicities.
2nd most effect of all antipsychotics.
Weight gain very problematic - Now 3rd line agent.

30
Q

Quetiapine characteristics

A 
Sedating
- Can be useful
Low EPS due to active metabolite
Low adrenergic blockade
Moderate weight gain / risk of metabolic syndrome
31
Q

Risperidone characteristics

A

Lack of sedation is attractive
Restlessness/agitation can be a problem though
Dose control to avoid EPS
Also approved for irritability in autism spectrum disorder at age 5 and up.

32
Q

Paliperidone characteristics

A

Hydroxy metabolite of risperidone
Similar profile including restlessness and EPS
Sustained release form leads to once monthly dosing.

33
Q

Ziprasidone and Lurasidone characteristics

A 
Low weight gain
Low EPS
Problems with QT elongation
- Less with Lurasidone
Cimetidine interaction with Ziprasidone
34
Q

Iloperidone characteristics

A 
Low EPS
Low anti-cholinergic effects
Low weight gain
Low tendency for metabolic syndrome
but
Hypotension is a problem - requires dose titration.
Caution 2D6/3A4 inhibitors.
35
Q

Asenapine characteristics

A

Minimal weight gain and metabolic disturbance.
Extreme sedation from H1-Antagonism.
Off label for PTSD.
Serious hypersensitivity reactions - anaphylaxis alert.
EPS concern due to low M1-Antagonism
May not be very efficacious anyways..
Weak 2D6 inhibitor

36
Q

Aripiprazole characteristics

A 
D2-Partial Agonist - 30%
Transient nausea
No endocrine disturbances
- Slight decrease in prolactin actually.
No receptor sensitization
- Low risk of EPS or TD
Good efficacy
but
May increase psychoses in a subset of patients
Agitating
Alpha-1-Antagonism - decrease BP, increase HR
Increasing reports of weight gain with time.
Very long t1/2 (EM/PM?)
37
Q

Brexpiprazole

A 
Newer
Weaker D2-partial agonist than Aripiprazole
Partial agonist at 5HT1A
Antagonist at 5HT2
Low risk for EPS or TD
Alpha-1-Antagonism
Low H-1 affinity
Common SE: Akathisia (agitation, distress, restlessness), moderate for weight gain.
38
Q

Cariprazine

A 
Newer
D2-partial (ant)?agonist
5HT1A Partial agonist
5HT2 Antagonist
D3 Partial agonist > D2!
EPS in 1/4 to 1/3 of patients...
Low weight gain
39
Q

Pimvanserin Indication

A

Parkinson’s associated psychoses

Phar 752 (12 decks)

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