Antipsychotics Flashcards by Kevin G

Benztropine- what is it?

Anti-cholinergic

treats EPS effects of antipsychotics

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Chlorpromazine- what is it?

Phenothiazine
Competitive antagonist at:
- Dopamine D2 (primary antipsychotic effect)
- Muscarinic cholinergic (anti-ACh AEs)
- Histamine H1
- alpha-adrenergic (orthostatic hypotension)
- 5-HT2

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Clozapine- what is it?

Atypical antipsychotic

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Diphenhydramine- what is it?

histamine H1 antagonist
- Also anti-cholinergic
(treats EPS effects of antipsychotics)

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Droperidol- what is it?

Pharmacologically very similar to haloperidol, but used as anti-emetic

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Fluphenazine- what is it?

Phenothiazine
Competitive antagonist at:
- Dopamine D2 (primary antipsychotic effect)
- Muscarinic cholinergic (anti-ACh AEs)
- Histamine H1
- alpha-adrenergic (orthostatic hypotension)
- 5-HT2

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Haloperidol- what is it?

High-potency (typical) Antipsychotic
Butyrophenone class

D2-antagonist
little antagonist activity at muscarinic or alpha-adrenoceptors (therefore little hypotension or sedation)

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Olanzapine- what is it?

Atypical antipsychotic

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Prochlorperazine- what is it?

Same as chlorpromazine, but used as anti-emetic so normal ppl don’t have to “take antipsychotics”

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Risperidone- what is it?

Atypical antipsychotic

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Thioridazine- what is it?

Phenothiazine
Competitive antagonist at:
- Dopamine D2 (primary antipsychotic effect)
- Muscarinic cholinergic (anti-ACh AEs)
- Histamine H1
- alpha-adrenergic (orthostatic hypotension)
- 5-HT2

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Trihexyphenidyl- what is it?

Anti-cholinergic

treats EPS effects of antipsychotics

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Trifluoperazine- what is it?

Phenothiazine
Competitive antagonist at:
- Dopamine D2 (primary antipsychotic effect)
- Muscarinic cholinergic (anti-ACh AEs)
- Histamine H1
- alpha-adrenergic (orthostatic hypotension)
- 5-HT2

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Quetiapine- what is it?

Atypical antipsychotic

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Ziprasidone- what is it?

Atypical antipsychotic

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Aripiprazole- what is it?

Atypical antipsychotic

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Why are atypical antidepressants described as “atypical”?

They have less (or no) antagonistic

activity at dopaminergic & cholinergic receptors

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What are “Neuroleptics”?

Another term for antipsychotics

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Chlorpromazine’s antipsychotic effect is thought to result from dopaminergic blockade in the _____ & _____.

prefrontal & limbic cortices

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Blockade of dopamine receptors in the basal ganglia leads to extrapyramidal effects, which are…? (4)

Akathisia
Dystonia
Rigidity
Tardive dyskinesia

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What is “Akathisia”?

An uncomfortable inability to sit still

Acute dystonic signs are usually manifested how?

As uncomfortable (and embarrassing) contractions of the muscles of the face and neck

The rigidity that occurs in antipsychotics may be clinically indistinguishable from that of _____.

Parkinson disease

How are the Extrapyramidal effects of antipsychotics treated?

Anticholinergics such as trihexyphenidyl, benztropine, or diphenhydramine

______ is characterized by involuntary, repetitive, | stereotyped movements usually of the face such as lip smacking, eye blinking, grimacing, or tongue protruding.

Tardive Dyskinesia

How often does Tardive Dyskinesia become permanent?

In up to half of the cases

What is Neuroleptic malignant syndrome?

A rare complication of chlorpromazine therapy and is characterized by hyperthermia (due to generalized muscle contracture), stupor, and such metabolic abnormalities as myoglobinemia and elevation of creatine kinase

Does tolerance develop to chlorpromazine?

No (nor to any of the antipsychotic agents)

(Antipsychotics) In general, those medications with a greater anticholinergic effect are __(a)__ sedating and __(b)__ likely to cause extrapyramidal effects.

a) more b) less (also tend to cause more orthostatic hypotension due to alpha-adrenergic blockade)

Thioridazine has __(a)__ sedating and hypotensive effects as compared with chlorpromazine while causing many __(b)__ extrapyramidal reactions.

a) greater | b) fewer

Trifluoperazine and fluphenazine are __(a)__ sedating, cause __(b)__ hypotensive effects, and are __(c)__ likely to cause extrapyramidal reactions than chlorpromazine

a) less b) fewer c) more

Which of the antipsychotics may cause QT prolongation?

Trifluoperazine

Does Haloperidol or have anticholinergic or anti-alpha-adrenergic activity?

No (or very little)

______ is commonly used for inpatients whose primary diagnosis is not psychosis but who require antipsychotic therapy (e.g., ICU-associated psychosis)

Haloperidol

What is the antipsychotic activity in atypical antipsychotics thought to be due to?

5HT2 blockade

Atypical antipsychotics: AEs? (that they all share)

- Orthostatic Hypotension (b/c they are potent alpha-antagonists)

Extrapyramidal effects of atypical antipsychotics?

EPS are much rarer in atypical antipsychotics than w/ older antipsychotics

Orthostatic hypotension in atypical antipsychotics?

This is a common problem due to their alpha-adrenergic antagonistic effects

Which of the atypical antipsychotics is a partial agonist at both dopaminergic D2 and 5-HT1A receptors.

Aripiprazole

_____ may cause weight gain, diabetes, seizures, & agranulocytosis

Clozapine

Clozapine: AEs?

- Orthostatic hypotension - weight gain - diabetes - seizures - agranulocytosis

______, although very closely related to clozapine in structure, does not cause seizures nor agranulocytosis; it may cause weight gain and diabetes.

Olanzapine

Olanzapine: AEs?

- Orthostatic hypotension - weight gain - diabetes

Which of the atypical antipsychotics may cause extrapyramidal effects at high doses & weight gain?

Risperidone

Which of the atypical antipsychotics may rarely cause extrapyramidal effects and QT prolongation (that may predispose some persons to cardiac dysrhythmias)?

Ziprasidone

Name the 3 atypical antipsychotics that don't cause weight gain.

Quetiapine, Ziprasidone, & Aripiprazole

Amongst all the antipsychotics, which is the most effective & which is the most toxic?

Clozapine is both

Behind Clozapine, which are the most effective antipsychotics?

Risperidone and olanzapine are the next best | & are superior to the phenothiazines and butyrophenones

Which of the antipsychotics are orally effective?

All of them | that we've learned about

For the emergency management of acute psychosis, __(a)__ may be given intravenously or intramuscularly b) What other 3 may also be given intramuscularly?

a) Haloperidol | b) Chlorpromazine, Ziprasidone, or Olanzapine

_____ should rarely be given intravenously because of its profound vasodilatory effect.

Chlorpromazine

For long-term management of patients that are non-compliant w/ oral therapy, which 3 antipsychotics may be prepared as a formula to be given as an intramuscular injection every few weeks?

Haloperidol, Fluphenazine, & Risperidone