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Pharmacology > Antipsychotics > Flashcards

Antipsychotics Flashcards

1
Q

What are antipsychotic drugs?

A

antipsychotics, also known as neuroleptics, are drugs used primarily to treat psychotic states such as schizophrenia, delusional disorder, and other hallucinatory states

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2
Q

What is MOA of antipsychotics?

A

Antipsychotics block various receptors including cholinergic, adrenergic, serotoninergic, muscarinic, and histamine receptors.
However, their antipsychotic actions are primarily thought to be due to blocking of DOPAMINE RECEPTORS in the CNS, particularly the D2 receptors in the mesocortical & mesolimbal systems of the brain.

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3
Q

Do antipsychotic agents differ in potency?

A

Yes - a drug’s parallels its affinity for D2 receptors.

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4
Q

Which antipsychotic drugs are high potency drugs because they have high affinity for D2 receptors

A

Haloperidol (Haldol)

Thiothixene (Mellaril)

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5
Q

Which antipsychotic agents are low-potency drugs because they have low affinity for D2 receptors?

A

Chlorpromazine (Thorazine)

Thioridazine (Mellaril)

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6
Q

Do antipsychotics diifer in efficacy?

A

NO. the traditional antipsychtoics are all considered to be equivalent in efficacy.

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7
Q

What is the onset of action of antipsychotic drugs?

A

Antipsychtotics may not become effective for several weeks to months. However, sedation and other side effects can occur rapidly

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8
Q

Can antipsychotic drugs cure illnesses such as schizophrenia?

A

NO! antipsychotics only reduce symptoms of illness; they cannot cure

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9
Q

How are antipsychotics classified?

A

Classification is based on structural differences. The major classes include phenothiazines:

  1. butyrophenones
  2. dibenzoxazepines
  3. thioxanthines
  4. benzisoxazoles
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10
Q

What are some examples of phenothiazines?

A
  1. Chloropromazine (Thorazine) - prototype
  2. Fluphenazine (Prolixin)
  3. Trifluoperazine (stelline)
  4. Thioridazine (Mellaril)
  5. Perphenazine (Trilafon)
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11
Q

What distinctive side effects does thioridazine (Mellaril) cause?

A

Pigmentary retinopathy

retinitis pigmentosa

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12
Q

Name two drugs int he class Butyrophenones

A
  1. Haloperidol (Haldol)

2. Droperidol (Inapsine)

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13
Q

Other psychotic states, for what can Haloperidol be used?

A

Tourette’s syndrome
Huntingtons Disease
Phencyclindine overdose - DRUG OF CHOICE

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14
Q

What type of side effects is especially pronounced with Haloperidol?

A

Extrapyramidal side effects!
–> Acute dystonia, Akathisia, parkisonism, tardive dyskinesia
COMMON BOARD QUESTION!

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15
Q

Name a drug that belongs to the Dibenzoxazepines

A

Loxapine (Loxitane)

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16
Q

Name a drug that belongs to the Thioxanthenes?

A

Thiothixene (Navane)

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17
Q

What are the clinical applications of traditional antipsychotic agents?

A

traditional neuroleptics have several therapeutic uses, but the most important to remember are:

  • Treatment of any agitated or psychotic state
    1. Bipolar disease
    2. Schizophrenia - effective for + symptoms such as delusions, thought disorders, and hallucinations
  • Antiemetic therapy - phenothiazines with the exception of thioidazine
  • Treatment of Tourette’s syndrome
  • Treatment of intractable hiccups
  • Antipruritic therapy
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18
Q

Treatment of Tourettes syndrome

A

Haloperidol

19
Q

Treatment of intractable hiccups

A

Chlorpromazine

20
Q

Treatment - Antipruritic therapy for antipsychotics

A

Promethazine (bc of histamine blockage)

21
Q

What is an easy way to remember the side effects of the traditional antipsychotics?

A

With a few exceptions, all of the traditional antipsychotics have similar toxicities - namely , sedation, extrapyramidal effects, anticholinergic effects, and alpha-adrenergic effects (hypotension).

22
Q

Which antipsychotics produce the greatest extrapyramidal effects

A

Haloperidol and Fluphenazine (Prolixin)

23
Q

Which antipsychotic drugs produce the greatest anticholinergic effects?

A

Thioridazine & Chlorpromazine

24
Q

Describe the toxicities of traditional antipsychotic agents

A
  1. CNS sedation (Markedly seen with phenothiazines)
  2. Endocrine alteration (galactorrhea, amenorrhea, and infertility, likely due to blockade of dopamine release from the pituitary)
  3. Antiadrenergic effects - (watch for light headedness and orthostatic hypotension secondary to alpha-adrenergic blockade. Phenothiazines can cause sexual dysfunction *FAILURE TO EJACULATE!!
  4. Extrapyramidal side effects - akathisia (most or restlessness); parkinsonian syndrome (bradykinic rigidity, tremor); acute dystonic reactions, neuroleptic malignant syndrome, and tar dive dyskinesia
    * **COMMON BOARD QUESTION
25
Q

What is tar dive dyskinesia

A

symptom that may occur after prolonged therapy with neuroletpics (4 months to 1 year). It is characterized by rhythmic involuntary movements of the tongue, lips, or jaw. Patients may also demonstrate puckering of the mouth or even chewing movements.

26
Q

Is tardive dyskinesia reversible?

A

There is no known treatment for established cases of tar dive dyskinesia. They symptom may remit partially or completely if neuroleptic treatment is withdrawn, although in many cases it is irreversible. Anticholinergic agents actually increase the severity of tardive dyskinesia.

27
Q

What is an acute dystonic reaction?

A

prolonged muscle spasms of tongue, neck, or face

28
Q

What are acute dystonic reactions treated?

A

Patients are given Diphenhydramine (Benadryl) or an injection of Benztropine.

29
Q

What is neuroleptic malignant syndrome?

A

Patients who receive neuroleptics for long-term treatment may experience rigidity, altered mental status, cardiac arrhythmias, hypertension, and life-threatening hyperpyrexia.

30
Q

What is the therapy for neuroleptic malignant syndrome?

A

This disorder is treated with Dantrolene , a skeletal muscle relaxant!
**COMMON BOARD QUESTION!

31
Q

Name 6 examples of atypical antipsychotic drugs

A
  1. Clozapine (clozaril)
  2. Risperidone (Risperdal)
  3. Olanzapine (Zyprexa)
  4. Aripiprazole (Abilify)
  5. Quetiapine (Seroquel)
  6. Ziprasidone (Geodon)
32
Q

Why are these drugs considered “atypical”?

A

They are newer and in addition to blocking dopamine receptors, atypical antipsychotics also produce significant therapeutic effects through the blockade of serotonin (5-HT2) receptors. They are also rarely associated with extrapyramidal side affects.

33
Q

Are they more effective than traditional antipsychotics?

A

Most physicians consider them a better choice for therapy because of their decreased side effects

34
Q

Describe the actions of clozapine

A

this agent is a dibenzodiazepine derivative. It differs from traditional antipsychotics in its potent blockade of serotonin (5-HT2) receptors, along with the usual dopamine blockade.

35
Q

What is clonazapine used for?

A

schizophrenia that are refractory to other neuroleptic drugs. It is especially effective in treating NEGATIVE SYMPTOMS of schizophrenia
- blunted emotion, withdrawal, reduced ability to form relationships

36
Q

side effects of clozapine

A

fewer extrapyrimidal side effects than traditional neuroleptics.

  • DOES CAUSE SEIZURES & DANGEROUS AGRANULOCYTOSIS
  • **common board question
    • weekly blood tests are required for patients receiving clozapine therapy.
  • although WEIGHT GAIN can occur with extended treatment of most antipsychotics, it is ESPEICLALY PROMINENT WITH CLOZAPINE. (this can lead to hypertension)
37
Q

Describe the actions of Risperidone (Risperdal).

A

benzisoxazole drug that, like clozapine, has a very high affinity for 5-HT2 receptors. It also has antidopaminergic D2 activity.

38
Q

What is the first line agent for the treatment of schizophrenia, since it is effective for both the positive and negative symptoms of the disease?

A

Risperidone (Risperdal)
The drug is also known to prolong QT intervals and therefore should be used with caution in patients who have abnormal QT intervals.

39
Q

Side effects of Risperidone (Risperdal)?

A

However, risperidone exhibits no anticholinergic effects and diminished extrapyramidal effects.
The drug is also known to prolong QT intervals and therefore should be used with caution in patients who have abnormal QT intervals.

40
Q

MOA of Olanzapine (Zyprexa)

A

blocks both dopamine and serotonin receptors

41
Q

Clinical use of Olanzapine (Zyprexa)

A

effective in the treatment of both positive and negative symptoms of schizophrenia, depression, or Obsessive-compulsion disorder (OCD)

42
Q

Side effects of Olanzapine (Zyprexa)

A

anticholinergic effects and othrostatic hypertension

HIGH RISK OF WEIGHT GAIN & METABOLIC SYNDROME!!!

43
Q

only antipsychotic drug used that is a partial agonist at D2 receptors

A

Aripiprazole (Abilify)

Pharmacology (6 decks)

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