Antipsychotics Flashcards

1
Q

What is the major dopaminergic tract that is the source of psychosis?

A

Mesolimbic tract

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2
Q

One theory says that too much dopamine can cause….

A

Schizophrenia

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3
Q

How does the binding affinity of the antipsychotic drug affect its dosing?

A

The greater the binding affinity for DA receptors, the smaller dose is needed for the antipsychotic effect

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4
Q

List the Low Potency FGAs

A

Chlorpromazine

Thioridazine
Perphenazine
Thiothixene

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5
Q

What % of DA receptors need to be blocked to produce a therapeutic effect? What about side effects in the nigrostriatal and tuberoinfundibular tracts?

A

Therapeutic: block 60-65% of D2 receptors in the mesolimbic tract

Side effects in nigrostriatal and tuberinfundibular tracts: above 80% D2 receptor blockage

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6
Q

Chlorpromazine

Adverse Effects

A

Dopamine - EPS or Tardive dyskinisia; increased prolactin

Muscarinic- blurred vision, urinary retention, dry mouth, constipation

Alpha 1 adrenergic – orthostasis

H1 - sedation; weight gain

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7
Q

List the High Potency FGAs

A

Haloperidol

Fluphenazine
Trifluoperazine

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8
Q

High Potency FGAs

Adverse effects

A

Dopamine- EPS and TD; hyperprolactinemia (galactorrhea, gynecomastia)

No H1, musc, alpha1 side effects!

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9
Q

Excess dopamine blockage in the Nigrostriatal pathway tends to cause…

A

ExtraPyramidal Symptoms

Tardive dyskinisia

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10
Q

Excess dopamine blockage in the Tuberoinfundibular pathway tends to cause…

A

Hyperprolactinemia

Gynecomastia, Galactorrhea
Low GnRH
Osteopenia (increased fractures)

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11
Q

List some SGAs

A

Clozapine

Risperidone
Quetiapine
Aripiprazole
Olanzapine
Asenapine
Ziprasidone
Iloperidone
Paliperidone
Luraisdone
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12
Q

SGAs

MOA

A

Dual antagonism of both the presynaptic 5HT-2A and postsynaptic D2 receptors

Blocking the 5HT-2A receptors causes a disinhibition of DA release, thus causing excess DA in the synapse, so SGA DA blockade is not as long lasting

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13
Q

Which SGA is a partial agonist of the DA receptor? Describes its pharmacodynamics

A

Aripiprazole

Has agonist effects in a low dopamine environment. Has antagonist effects in a high dopamine environment

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14
Q

Positive Results of using Clozapine (a SGA)

A

Has efficacy in treating negative symptoms of schizophrenia

Helps with TD

Decrease risk of suicide or violence

Helps with treatment resistant schizophrenia

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15
Q

Clozapine is the 3rd line choice for antipsychotics (after 2 others failed). This is due to its adverse effects, including…

A

Common: Sedating, Weight Gain
Metabolic Syndrome
Anticholinergic

Rare:
AGRANULOCYTOSIS
Myocarditis
Decreased Seizure threshold

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16
Q

All antipsychotics have the potential side effect of NMS. What is that?

A

NMS = Neuroleptic Malignant Syndrome

Caused by excess dopamine blockade

Dopamine system goes haywire, causing mental status changes, rigidity, tremor, fever, inc HR, low BP, inc RR

17
Q

What is the recommendation for treating elderly patients with antipsychotics?

A

Treat with low doses for minimal time

FGAs and SGAs can cause sudden death in elderly patients with dementia

18
Q

Which SGA has the longest half life?

A

Aripiprazole (3 days)

19
Q

Describe the protein binding of Antipsychotics

A

90% protein bound, unbound portion passes through the BBB

20
Q

Avg half life for antipsychotics

A

About 30 hours (so you reach steady state between 4-7 days)

21
Q

What is the only treatment for Tardive Dyskinisia?

A

Clozapine

22
Q

Aripiprazole

Adverse Effects

A

Dopamine- akathesia

Low risk of weight gain

Musc, Adrenergic, H1– none

23
Q

What is the relationship between Risperidone and Palliperidone?

A

Risperidone is metabolized to Palliperidone

24
Q

Palliperidone

Excretion

A

Mostly renally excreted, so used in pts with liver disease

25
Q

What is special about the administration of Ziprasidone and Lurasidone?

A

MUST be taken with food (improves absorption by 50%)