Antipsychotics Flashcards

1
Q

What are extrapyramidal symptoms (EPS)?

A

Motor side effects due to blocking dopamine (D2) receptors

  • Dystonia (continuous spasms and muscle contractions)
  • Akathisia (motor reslessness)
  • Parkinsonism (characteristic symptoms susch as rigidity, bradykinesia, and tremor)
  • Tardive dyskinesia (irregular, jerky movements)
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2
Q

What is a general rule for determining if a drug causes EPS (neurologic motor) symproms or metabolic symptoms?

A
  • -pines: Metabolic risk
  • -dones/-oles” EPS (motor neurologic)
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3
Q

What are the four dopaminegeric pathways?

A
  • Mesocortical (VTA → cortex)
  • Nigrostriatal (substantia nigra → striatum) - Control of movement
  • Mesolimbic (VTA → limbic system)
  • Tuberoinfundibular (hypothalamus → pituitary) - Inhibits prolactin release
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4
Q

Antipsychotic medications are clinically indicated for use in what three situations?

A
  • Schizophrenic psychosis
  • Antiemesis
  • Hiccups
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5
Q

What results in negative symptoms in Schizophrenia?

A

Hypoactivity of the mesocortical pathway

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6
Q

What causes positive symptoms in Schizophrenia?

A

Hyperactivity of the mesolimbic system

  • Main target for antipsychotics
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7
Q

Blockade of the nigrostriatal pathway results in what?

A

Extra-pyramidal symtoms (EPS)

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8
Q

Blockade of the mesolimbic system results in what?

A

Antipsychotic effect (main target)

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9
Q

Blockade of the mesocortical pathway may result in what?

A

May worsen negative symptoms

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10
Q

What receptor is the main target for antipsychotics?

A

Blockade of the dopamine D2 receptor

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11
Q

Blockade of the tuberoinfundibular pathway results in what?

A

Hyperprolactinemia

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12
Q

(Thioridazine/Chlorpromazine/Fluphenazine) is capable of stopping intractable hiccups.

A

Chlorpromazine

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13
Q

Blockade of the chemoreceptor trigger zone/area postrema results in what?

A

Blockade reduces vomiting

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14
Q

What percentage of D2 receptors need to be blocked to see an antipsychotic effect?

A

60 - 80 %

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15
Q

Which antipsychotics have a “fast-off” (short acting) property?

A
  • Quetiapine (doesn’t occupy 60% of D2 receptors)
  • Clozapine

Works as antipsychotic with little to no EPS

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16
Q

Which antipsychotic acts as a partial agonist at low concentrations but an antagonist at high concentrations?

A

Aripiprazole

17
Q

What are some unique feature of aripiprazole?

A
  • Actually has increased nausea (via D2 agonism)
  • Can lower prolactin
  • Very expensive
18
Q

Resistant OCD with or without tourettes can be treated with whcih antipsychotic?

A

Risperidone

19
Q

What is the most effective drug for schizophrenia?

A

Clozapine (by far, just has adverse side effects)

20
Q

What are some advantages of clozapine?

A
  • Very efficatious for Schizophrenia
  • Some efficacy against negative symptoms
  • Does NOT cause EPS at all (can even be used in Parkinsons patients with psychosis
  • Does NOT cause tardive dyskinesia (and may even improve)
  • Social stimulus improves
21
Q

Which adverse motor effects typically occur early in treatment with antipsychotics?

A
  • Acute dystonia (1-5 days)
  • Akathisia (5-60 days)
  • Parkinsonian syndrome (5-30 days)
22
Q

Which adverse motor effects typically occur late in treatment with antipsychotics, sometimes taking months or years to develop?

A
  • Tardive dyskinesia
  • Perioral tremors (tremors around the mouth; Rabbit syndrome)
23
Q

What are the adverse effects of clozapine?

A
  • Agranulocytosis
  • Seizures
  • DKA, cadriomyopathy, pulmonary embolism, bowel obstuction
  • Weight gain

Worst metabolic symptoms

24
Q

Which antipsychotics cause the most weight gain?

A
  • Clozapine
  • Olanzapine

Cloz Olaz of metabolic symptoms

25
Q

Whic antipyschotics have the greatest increase of prolactin?

A
  • Risperidone
  • Paliperidone

Results in decrease of GnRH, LH, and FSH (casuing irregular menstation and fertility issues)

Increased prolactin can cause gynecomastia, glactorrhea

26
Q

How is acute dystonia treated?

A

Acute dystonia - Torticollis (wry neck), oculogyric crisis (upward elevation of eyes), really painful muscle spasms

  • Benztropine
  • Diphenhydramine
27
Q

How is Parkinsonism treated?

A

Parkinsonism - TRAPS (Tremor (at rest), cogwheel Rigidity, Akinesia (bradykinesia), Postural instability, Shuffling gait)

  • Benztropine
28
Q

What is the difference between idiopathic Parkinson’s and Parkinsonism?

A
  • Idiopathic Parkinson’s - Unilateral
  • Parkinsonism - Bilateral
29
Q

What is the treatment for akathisia?

A

Akathisia - Uncomfortable resltlessness

  • Propanolol
30
Q

What is the treatment for tardive dyskinesia?

A

Tardive Dyskinesia - Involvuntary movements: Tongue thrusting and chewing movements, face coiling, chorieform movemetns, etc.

  • Not much can be done for treatment (prevention is best)
31
Q

What are the symptoms of Neuroleptic Malignant Syndrome (NMS)?

A

FEVER

  • Fever (105-106ºF)
  • Encephalopathy
  • Vitals unstable
  • Enzymes ↑ (CK; also elevated WBC (leukocytosis) and myoglobinuria)
  • Rigidity of muscles
32
Q

How is Neuroleptic Malignant Syndrome (NMS) treated?

A
  • Stop drug(s) causing it
  • ICU management
  • Dantrolene
  • D2 agonist (bromocriptine)
33
Q

What are the side effects of Chlorpromazine (1st gen antipsychotic)?

A
  • Anticholinergic side effects
    • Dry mouth, blurred vision, constipation
  • Antihistaminic side effects
    • Sedation and weight gain
  • Alpha1 blockade
    • Orthostatic hypotension
34
Q

Which antipsychotic has the worst neurologic side effects?

A

Haloperidol

  • EPS
    • Dystonia
    • Akathisia
    • Tardive dyskinesia
  • ↑ QTC
  • ↑ Prolactin
35
Q

What can be given to patients that are non-adherent in taking their medications?

A

Haloperidol decanoate, Fluphenazine deconoate, Risperidone microspheres, Paliperidone palmitate

  • Anything with two words in the name
36
Q

Which antipsychotics can increase the QTC interval?

A
  • Ziprasidone
  • Quetiapine
  • Haloperidol