Antipsychotic Drugs Flashcards

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1
Q

All drugs capable of reducing psychosis, to date, are antagonists of these receptors:

A

D2

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2
Q

Blocking D2 receptors is thought to relieve positive or negative symptoms?

A

Positive

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3
Q

Lower affinity for ____ receptors reduces extrapyramidal side effects. This is seen with 1st or 2nd gen (atypical) antipsychotics?

A

D2

atypicals (2nd gen)

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4
Q

Although 2nd gen antipsychotics (atypicals) are proported by drug companies to relieve negative symptoms of psychosis (derangements of normal function such as flat affect, etc.), they really only work (as shown clinically) to improve these symptoms:

A

Positive (delusions, hallucinations, etc.)

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5
Q

Due to their effect on these receptors, antipsychotics produce some ADEs such as orthostatic hypoTN, tachycardia, sedation, confusion, and memory impairment:

A

a1- orthostatic hypoTN, tachycardia
H1- sedation
M1,2,3- confusion, memory impairment

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6
Q

Which antipsychotics (class) produces EPS?

A

Typicals

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7
Q

Which antipsychotics (class) is known to elevate prolactin levels?

A

Typicals

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8
Q

Chlorpromazine, low or high potency?

A

Low

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9
Q

Thiothixene, low or higher incidence of EPS?

A

Low

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10
Q

Fluphenazine and perphenazine, low or high potency?

A

High potency

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11
Q

ADEs of Chlorpromazine and thiothixene?

A

antimuscarinic effects. Low incidence of EPS

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12
Q

ADEs of Fluphenazine and perphenazine?

A

Incr. risk of EPS and weak anti-ACh effects

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13
Q

Haloperidol, high or low potency?

A

High

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14
Q

Clozapine, high or low potency?

Typical or atypical?

A

Low

Atypical

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15
Q

Only agent approved for use in kids/teens?

A

Risperidone

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16
Q

Risks associated w/ high dose risperidone?

A

EPS seen with high doses of risperidone bc at high doses it acts like a TYPICAL even though it is ATYPICAL

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17
Q

MOA of risperidone?

A

5-HT/D2 antagonism

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18
Q

Which atypical antipsychotic is a partial agonist, and thus shows lesser R/O ADEs?

A

Aripiprazole- D2 partial agonist

Also a 5-HT2A antagonist and 5-HT1A partial agonist

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19
Q

This antipsychotic is an antagonist of D1/D2, 5-HT1/2A and a1 AND H1!
High or low affinity for M1, 2, 3 receptors?

A

Asenaprine

Low affinity for muscarinic receptors

20
Q

What characterizes neuroleptic syndrome?

DO NOT CONFUSE W/ NEUROLEPTIC MALIGNANT SYNDROME (NMS)

A

Suppression of spontaneous movements (parkinsonism)
Reduced initiative and interest in environment
Decr. manifestations of emotion or affect

  • psychotic symptoms disappear w/ time
21
Q

What part of the brain to antipsychotics act on?

A

limbic system- remember bc DA is most concentrated here!

22
Q

The EPS of antipsychotics (mostly typicals) are thought to be derived from D2 antagonism here in the brain:
What drug can we give to overcome this?

A

Basal ganglia

Tx EPS w/ anticholinergics (Benztropine)
Unlike in the limbic system, anticholinergics block anti-psychotic induced increases in DA turnover in the basal ganglia, which helps restore balance tipped by DA secretion to overcome D2 antagonism in the basal ganglia.

23
Q

Describe EPS

A
Acute dystonia
Akasthesia- can't stop moving "ants in pants"
Parkinsonian syndrome
NMS
Perioral tremor
Tardive dyskinesia
24
Q

Tx for akasthesia?

A

decr. dose
antiparkinsonians
anxiolytic like propranolol

25
Q

Why not give L-dopa for parkinsonian syndrome?

What do you give, then?

A

NO- induces agitation and enhances psychosis

Give: anticholinergics, amantadine

26
Q

Describe NMS. Tx?

A

Severe parkinsonism + catatonia
Fever, myoglobinemia, elev. CK, autonomic instability
10% mortality! Stop drugs immediately!

Tx: bromocriptine, dantrolene, supportive care

27
Q

Pt has a perioral tremor due to antipsychotics, what do you do?

A

Stop antipsychotics, give anticholinergic

28
Q

Pt has tardive dyskinesia. Tx?

A

STOP ANTIPSYCHOTIC
Symptoms fade w/ time (or don’t).
No adequate tx

29
Q

Why can pts on antipsychotics be at greater R/O seizures?

Which one in particular?

A

Some antipsychs can lower seizure threshold

Clozapine

30
Q

DA is stimulating the chemo trigger zone causing N/V. What can you tx with?

A

Typical antipsychotics

31
Q

What effect to antipsychs have on the hypothalamus and what terminal effects does this have on the pt, clinically?

Avoid this in pts w/:

A

^^ PRL secretion —> v FSH/LH levels—> amennorhea, galactorrhea, gynecomastia, sexual dysfunction, hypoestrogenism/osteopenia

Avoid in pts w established breast carcinoma

32
Q
Regarding the ^^ PRL levels of antipsychotics, which class is known to cause this the most?
Why?
A

Typicals

- due to blocking D2 receptors which normally inhibit PRL secretion!

33
Q

Which TYPICAL antipsychotic is associated with development of glucose intolerance and decr. insulin release?

A

Chlorpromazine

34
Q

Which Atypical antipsychs are associate with incr. rise of T2DM?

A

All ATYPICALS to some extent, but especially:

Clozapine and Olanzepine

35
Q

Which antipsychs are associated with prolonged QTc?

A

Low potency typicals: chlorpromazine and thioridazine

36
Q

Which antipsych can cause jaundice?

Why does this occur?

A

Chlorpromazine - this typical seems to really suck with the side effects
It is a hypersensitivity reaction.

37
Q

Your pt is on clozapine. You will need to get weekly blood tests to observe for this ADE:

A

Leukopenia—> AGRANULOCYTOSIS

Other blood dyscrasias: leukocytosis, eosinophilia

38
Q

Your psych pt presents with a skin rash you assume to be caused by this antipsychotic you have them on:

A

a phenothiazine: (chlorpromazine, of course)

39
Q

You need to put your pt on an antipsych for the long-term. Which class should you avoid and why?

A

Avoid Atypicals because of incr. chance of endocrine dysfunction–> weight gain –> CVD

40
Q

Describe the mechanism of weight gain seen in atypical antipsychs.

A

histaminergic and serotonergic blockade

41
Q

Give antipsychs to a carrying or breastfeeding mother?

A

No. They cross placental barrier and enter breast milk.

42
Q

With these exceptions, antipsychs are broken down into inactive metabolites.

A

Chlorpromazine–> 7-OH-Chlorpromazine
Risperidone–> Paliperidone
Aripiprazole–> Dehydroaripiprazole

43
Q

Your pt complains about the sedatives effects of the antipsych you have them on. What should you do/tell them?

A

Keep them on it.

They will gain a tolerance to the effects over days-weeks

44
Q

Due to their inhibition of this enzyme, antipsychs are known to raise serum levels of TCAs and SSRIs.

A

CYP2D6

45
Q

You don’t think your psych pt will reliably take their antipsychotic meds orally. What is another option to better ensure your pt is properly treated?

A

Depot shots IM