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PHRM 845 > 53 - Pharmacology of antipsychotic drugs > Flashcards

53 - Pharmacology of antipsychotic drugs Flashcards

1
Q

Drug-Induced Movement Disorders D2 Antagonism

Extrapramidal Symptoms (EPS) 30-50%
- occur early, days/weeks, ___

Symptoms
- dystonia - ___ muscle tone
- pseudoparkinsonism - muscle ___
- tremor
- akathisia - ___

unfortunately most patients will experience EPS as a results of ___ antipsychotic drug therapy

A
  • reversible
  • increased
  • rigidity
  • restlessness

long-term

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2
Q

Drug therapy for EPS

  • Anticholinergic agents: ___ (Cogentin), ___ (Artane), or ___ (Biperiden)
  • Antihistamine - ___ (Benadryl)
  • dopamine releasing agent - ___ (Symmetrel)
  • ___ - used for akathisia
A
  • benztropine, trihexyphenidyl, akineton
  • diphenhydramine
  • amantadine
  • propranolol
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3
Q

Drug-Induced Movement Disorders D2 Antagonism

Tardive Dyskinesia (20-40%)
- occur late, months to a year and is ____
- mouth - rhythmic involuntary movements
- choreiform- irregular purposelessness
- athetoid - worm like
- axial hyperkinesias - to and fro movements

Monitoring: ____ (Abnormal Involuntary Movement Scale), check every 6 months

Treatment: prevention! use the least risky agent at the ___ dose possible and monitor
- reduce dose of current agent
- change to a different drug (possibily a newer agent)
- eliminate ____ drugs
- ___ inhibitors

A
  • irreverisble
    AIMS
    lowest
    anticholinergic
    VMAT
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4
Q

Drug-Induced Movement Disorders D2 Antagonism

Tardive Dyskinesia (20-40%)
- occur late, months to a year, and ____
- mouth - rhythmic involuntary movements
- choreiform - irregular purposelessness
- athetoid - worm like
- axial hyperkinesias - to and fro movements

unknown MOA: antagonist ___ of receptors to dopamine (?)

A
  • irreversible
  • supersensitivity
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5
Q

Tardive Dyskinesia

newer drug therapies for TD: ___ inhibitors
- ____ (Xenazine) for Huntington’s chorea
- ____ (Ingrezza) for TD
- ___ (Austedo) for TD and Huntington’s chorea

A

VMAT2
- tetrabenazine
- valbenazine
- deutetrabenazine

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6
Q

Drug-Induced Movement Disorders D2 Antagonism

TD (cont.)
monitoring: ___ (abnormal involuntary movement scale); check rating scale every 6 months

treatment: ___ ! use the least risky agent at the lowest dose possible and monitor
- reduce dose
- change to different (newer) drug
- eliminate ___ drugs
- ___ inhibitors

A

AIMS
prevention
- anticholinergic
- VMAT

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7
Q
A
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8
Q

Drug-Induced Movement Disorders D2 Antagonism

newer drug therapies for TD:
- ___ (Xenazine) for Huntington’s chorea
- ___ (Ingrezza) for TD
- ___ (Austedo) for TD and Huntington’s chorea

A

tetrabenazine
valbenazine
deutetrabenazine

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9
Q

Drug-Induced Movement Disorders D2 Antagonism

Neuroleptic Malignant Syndrome (NMS)
- serious and ___ ; 10% fatality

symptoms
- EPS with fever
- impaired cognition
- muscle rigidity

treatment: restore ___ balance
- d/c drug
- DA ___ , diazepam, or dantrolene (skeletal muscle relaxant)

A
  • fatal
  • dopamine
  • agonist
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10
Q

MSC use

Tourette’s syndrome
- tics/vocalizations
- ___ (Orap)

A

Pimozide

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11
Q

MSC use

Huntington’s chorea
- ___ (Xenazine)
- ___ (Austedo)

A
  • tetrabenazine
  • deutetrabenazine
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12
Q

MSC use

alcohol withdrawal (Hallucinations)
- ___ (Haldol)

A

Haloperidol

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13
Q

MSC use

N/V
- ___ (Reglan)
- ___ (Phenergan)

A
  • metoclopramide
  • promethazine
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14
Q

MSC use

potentiation of opiates/sedatives
- ___ (Inapsine)

A

droperidol

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15
Q

PCOL effects of antipsychotic drugs

behavioral effects: reversal of signs and symptoms of ___ in affected individuals

neuroleptic syndrome: ___ emotions, reduce interest, may resemble ___ symptoms

decreased spontaneous activity, aggressive, and impulsive behavior

A
  • psychosis
  • suppress, negative
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16
Q

AE - autonomic

  • loss of accomodation, dry mouth, difficulty urinating, constipation = ____ receptor blockade
  • orthostatic hypotension, impotence, failure to ejaculate = ___ receptor blockade
A
  • cholinergic
  • alpha
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17
Q

AE - CNS

  • Parkinson’s syndrome, akathisia, dystonias = ___ receptor blockade
  • tardive dyskinesia = ___ of dopamine receptors
  • toxic-confusional state = ___ blockade
  • sedation = ___ receptor blockade
A
  • dopamine
  • supersensitivity
  • cholinergic
  • histamine
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18
Q

AE - endocrine system

amenorrhea, galactorrhea, infertility, impotence = dopamine receptor blockade resulting in ___

A

hyperprolactinemia

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19
Q

AE - other

weight gain = possibly combines ___ and ___ blockade

A

H1, 5HT 2C

20
Q

precautions and contraindications

  • CV
  • PD
  • epilepsy ( ___ will lower seizure threshold)
  • ___ (newer agents)
A

clozapine
diabetes

21
Q

1st Gen antipsyschotics

  • more ___ problems
  • increased EPS and TD due to strong ___ block
A

movement
D2

22
Q

1st Gen antipsyschotics

1st antipsychotic: ___

A

chlorpromazine

23
Q

1st Gen antipsychotics - phenothiazine nucleus

aliphatic phenothiazines
- ___ (Thorazine) - no longer 1st line therapy
- promezine (Sparine)
- Triflupromazine (Vesprin)

used for H1 antagonist properties
- ___ (Phenergan) - indicated for N/V
- trimeprazine (Temaril)

A
  • chlorpromazine
  • promethazine
24
Q

1st Gen antipsychotics - phenothiazine nucleus

piperidine phenothiazines
- ___ (Mellaril) - sedation, hypotension, anticholinergic, many SE
- mesoridazine (Serentil)

A

thioridazine

25
Q

1st Gen antipsychotics - phenothiazine nucleus

piperazine phenothiazines
- ___ (Permitil, Prolixin) - EPS
- trifluoperazine (Stelazine) - EPS
- ___ (Compazine) - antiemetic
- thiethylperazine (Torecan) - antiemetic
- ___ (Trilafon) - CATIE studies

A
  • fluphenazine
  • prochlorperazine
  • perphenazine
26
Q

1st Gen antipsychotics

thioxanthines
- ___ (Navane) - modest EPS
- chlorprothizene (Taratan)

A
  • thiothixene
27
Q

1st Gen antipsychotics

Butyrophenones
- ___ (Haldol) - EPS
- droperidol (Inapsine) - highly ___ , anxiolytic
- droperidol with fentanyl (Innovar)

A
  • haloperidol
  • sedative
28
Q

Miscellaneous Antipsychotics

___ (Moban)
- moderate EPS

___ (Orap)
- Tourette’s disease-tics, vocalizations

A

molindone
pimozide

29
Q
A
30
Q

atypical/2nd Gen antipsychotics

reduced EPS
- efficacy for ___ symptoms (?)
- similar or enhanced ___ receptor antagonism vs D2

more metabolic problems
- linked to ___ (greater risk in patients < 50)
- ___ and ___ (less evidence in quetiapine and risperidone)

A
  • negatove
  • 5HT2A
  • diabetes
  • olanzapine, clozapine
31
Q

atypical/2nd Gen antipsychotics

___ (Clozaril)
- 1st atypical
- very effective

agranulocytosis
- occurs in 1-2% within 6 months (weekly blood monitoring)
- 2nd or 3rd line therapy

SE: anticholinergic, antihistamine
- reduced ___ potency = ___ movement disorders
- risk of ___

A

clozapine
D2, decreased
diabetes

32
Q

atypical/2nd Gen antipsychotics

___ (Zyprexa)
- weight ___
- less likely to cause N/V
- less likely to cause ___ disorders
- risk of ___

A

olanzapine
- gain
- movement
- diabetes

33
Q

atypical/2nd Gen antipsychotics

___ (Loxitane)
- older agent
- metabolite = ___ (Ascendin)
- inhibits ___ = antidepressant

A

loxapine
amoxipine
NET

34
Q

atypical/2nd Gen antipsychotics

____ (Seroquel)
- metabolite with ___ activity
- 5HT2A and D2 (low ___ activity)
- low EPS
- ___ (a1)
- ___ (H1)
- risk of ___

A

Quetiapine
- antidepressant
- antimuscarinic
- hypotension
- sedation
- diabetes

35
Q

atypical/2nd Gen antipsychotics

___ (Risperidol)
- specifically and structurally designed to be both a ___ and ___ receptor antagonist!
- relatively low EPS with < 8 mg/day
- weight ___ ; some ___

A

risperidone
- 5HT2A, D2
- gain, sedation

36
Q

atypical/2nd Gen antipsychotics

___ (Invega)
- 9-hydroxy ____

___ (Fanapt)
- structurally related to ___
- very potent at ___ receptors
- 0.5 nM vs 5 nm at 5HT2A and D2

A

paliperidone
- 9-hydroxyrisperidone

iloperidone
- risperidone
- a1

37
Q

atypical/2nd Gen antipsychotics

___ (Geodon/Zeldox)
- affinity for ___ , ___ , and ___
- prolongs ___ interval

A

ziprasidone
- 5HT2A, D2, a1
- QTc

38
Q

atypical/2nd Gen antipsychotics

___ (Saphris)
- ___ and ___ (nM affinity at most 5HT, a, DA, and histamine receptor)

A

asenapine
- 5HT2A, D2

39
Q

atypical/2nd Gen antipsychotics

___ (Latuda)
- ___ and ___
- less weight gain and metabolic effects compared to ___
- ___ onset (days without titration)
- low doses have similar effectiveness to high doses

A

lurasidone
- 5HT2A, D2
- olanzapine
- fast

40
Q

atypical/2nd Gen antipsychotics

___ (Nuplazid)
- inverse agonist 5HT2A (40x more than 5HT2C)
- used for ___ disease psychosis

A

pimavanserin
Parkinson

41
Q

atypical/2nd Gen antipsychotics

___ (Abilify)
- high affinity for ___ and ___ (D2 actions are dopaminergic-state dependent and/or it is functionally selective)
- partial agonist at ___ receptors (being used for depression)
- moderate affinity for ___, ___, and ___ receptors
- side effects: weight ___ , low risk for D2 effects
- prodrug: ___ , given q 4-8 weeks

A

aripiprazole
- 5HT2, D2
- 5HT1A
- D4, a, histamine
- gain
- aripiprazole lauroxil

42
Q

dopaminergic activity - aripiprazole

dependent actions (partial agonism)

A

D2 actions are dopaminergic-state dependent and/or it is functionally selective

43
Q

D2/D3 receptor partial agonists

___ (Rexulti)
- D2/D3 partial agonist with supposedly less ___ vs aripiprazole
- indicated for schizophrenia and adjunct to antidepressants for major depression
- partial agonist activity at ___ and ___ receptors, and antagonist activity at ___ receptors

A

brexpiprazole
akathisia
5HT1A, D2, 5HT2A

44
Q

D2/D3 receptor partial agonists

___ (Vraylar)
- greater affinity for ___
- weak partial agonist activity at ___
- ___ is high
- for schizophrenia, mania, bipolar disorder

A

cariprazine
- D3
- 5HT1A
- akathisia

45
Q

D2/D3 receptor partial agonists

___ (Caplyta)
- partial ___ agonist at presynaptic receptors
- antagonist at postsynaptic receptors ( ____ antagonist)

A

lumateperone
- D2
- 5HT2A

46
Q
A

PHRM 845 (62 decks)

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