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iTx ii > Antipsychotics/EPS treatment > Flashcards

Antipsychotics/EPS treatment Flashcards

pharmacology/Medicinal Chemistry (49 cards)

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1
Q

Butyrophenones

A

-Droperidol
-Haloperidol

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1
Q

First Generation

A

Typical antipsychotics
-Butyrophenones
-Diphenylbutylpiperidine
-Phenothiazines

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2
Q

Diphenylbutylpiperidine

A

-fluspirilene
-penfluridol
-pimozide

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3
Q

Phenothiazines

A

Chlorpromazine
fluphenazine
thioridazine

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4
Q

Second Generation

A

Atypical antipsychotics

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5
Q

Atypical antipsychotics

A

aripiprazole, clozapine, risperidone, brexpiprazole, cariprazine, pimavanserin, latuda

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6
Q

What are the four main properties of second gen. antipsychotics?

A
  1. less/fewer EPS
  2. less prolactinemia
  3. moa involves D2 blockade as well as 5-HT2 blockade
  4. more efficacy for neg. sx
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7
Q

All antipsychotics are antagonists for which receptor?

A

Dopamine D2 receptors

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8
Q

Clozapine blocks which Dopamine receptor?

A

D4

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9
Q

At what percentage occupancy of D2-receptors is needed for therapeutic effect

A

80%

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10
Q

What rare and serious idiosyncratic reaction do some antipsychotics cause?

A

agranulocytosis

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11
Q

What is a common side effect of Clozapine that causes routine monitoring?

A

Leukopenia

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12
Q

D2 receptor blockade causes…

A

EPS and movement disorder, sexual dysfunction, endocrine SE (prolactin elevation)

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13
Q

5-HT1 receptor blockade causes…

A

ejaculatory disturbances

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14
Q

5-HT2 receptor blockade causes…

A

hypotension, wt gain, reduced sexual dysfunction, insomnia

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15
Q

blockade of AcH receptor causes…

A

blurred vision, dry mouth, sinus tachycardia, constipation, urinary retention, memory difficulties, anti-EPS side effects

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16
Q

H1 receptor blockade causes…

A

sedation, wt gain, anti-EPS side effects

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17
Q

alpha-1 adrenergic receptor blockade causes…

A

orthostatic hypotension, dizziness, syncope, reflex tachycardia, sedation, priapism

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18
Q

Chlorpromazine

A
  • dopamine antagonist
    -low potency
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19
Q

Chlorpromazine is used to treat what diagnoses?

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A

acute and chronic psychoses including schizophrenia and manic phase of bipolar disorder, amphetamine-induced psychoses

20
Q

chlorpromazine VERY COMMON adverse effects

Study These Flashcards
A

sedation, somnolence eps, wt. gain, orthostatic hypotension, dry mouth, constipation

21
Q

Chlorpromazine COMMON adverse effects

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A

ecg changes, contact dermatitis, photosensitivity, urticaria, maculopapular, petechial or edematous reactions, hyperprolactinaemia, impaired thermoregulation, hyperglycemia, etc.

22
Q

Chlorpromazine UNCOMMON adverse effects

Study These Flashcards
A

miosis, urinary retention, nasal congestion, nausea, obstipation, arrhythmias, skin pigmentation, etc.

23
Q

Chlorpromazine RARE adverse effects

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A

agranulocytosis, hemolytic anemia, aplastic anemia

24
UNKNOWN FREQUENCY adverse effects of Chlorpromazine
leucopenia, eosinophilia, pancytopenia
25
Haloperidol
- an inverse agonist of dopamine - high potency antipsychotic
26
Haloperidol can be used to treat what diagnoses?
- treatment of acute psychosis, severe behavior disorders
27
Haloperidol COMMON adverse effects
EPS, dystonia, muscle rigidity, akathisia, Parkinsonism, hypotension, constipation, dry mouth, blurred vision and somnolence
28
Haloperidol RARE adverse effects
jaundice, hepatitis, cholestasis, acute hepatic failure, hyperglycemia, anaphylactic reaction, hypersensitivity, agranulocytosis, etc.
29
Haloperidol UNKNOWN FREQUENCY adverse effects
prolonged Qt interval, orthostatic hypotension, increased respiratory rate, anemia, visual disturbances, HA, etc.
30
Haloperidol Limitations
-1/2 pts of schizophrenia fails to respons -limited efficacy against 1) neg. sx, 2) affective sx, 3) cognitive deficits -high proportion of patients relapse -SE and compliance issues -some safety issues are prominent
31
Atypical antipsychotics
- MARTA - SDA - Selective D2/D3 antagonists - D2/D3 agonists
32
MARTA (multi-acting receptor targeted agents)
- clozapine - olanzapine - quietiapine
33
SDA (serotonin-dopamine antagonists)
risperidone, ziprasidone
34
Selective D2/D2 antagonists
aripiprazole
35
D2/D3 partial agonists
Brexpiprazole (Rexulti) Cariprazine (Vraylar)
36
Clozapine
selectively blocks D2 receptors more strongly blocks 5-HT receptors in cortex which then acts to modulate some dopamine active
37
Clozapine adverse effects
- orthostatic hypotension effects, sedation, wt. gain, increased HR - increased risk for seizures (2-3%) - agranulocytosis in 1% - Agranulocytosis risks increase when co-administered with carbamazepine - itxns with SSRIs and valproic acid increase clozapine levels and risks
38
Ziprasidone
- 5th atypical antipsychotic - antagonist/inverse agonist of 5-HT. dopamine receptor, adrenergic receptor, mACh receptor, and NE transporter
39
Ziprasidone is used to treat what?
schizophrenia, acute mania and mixed states associated with bipolar disorder
40
Ziprasidone VERY COMMON adverse effects
somnolence, HA
41
Ziprasidone COMMON adverse effects
dizziness, dyspepsia, dry mouth, EPS, blurred vision, south, etc.
42
Ziprasidone UNCOMMON adverse effects
abnormal gait, thirst, palpitation, hyperprolactinemia, etc.
43
Ziprasidone RARE adverse effects
chest pain, feeling hot, pyrexia, sluggishness, gastroesophageal reflux, etc.
44
Brexpiprazole
atypical antipsychotic - partial agonist of D2 dopamine receptor - Serotonin-dopamine activity modulator (SDAM)
45
Brexpiprazole is used to treat what diagnoses?
schizophrenia, depression and major depressive disorder (MDD)
46
Enzyme Inhibition
decreased drug clearance --> system accumulation = TOXICITY
47
Enzyme induction
increased drug clearance --> decreased systemic drug level = treatment failure
48
what can be filtered by Ro5?
particles that fall under: - molecular wt < 500 Daltons - Lipophilicty LogP <5 - H-bond donors <5 - H-bond acceptors <10

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