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DRUGS > 12 - ANTIPYCHOTIC DRUGS > Flashcards

12 - ANTIPYCHOTIC DRUGS Flashcards

1
Q

Typical antipsychotics (classical)

A

They ae antagonists of D2 receptors: D2 blockade
CHLORPROMAZINE
HALOPERIDOL, DROPERIDOL

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2
Q

CHLORPROMAZINE

A

Typical antipsychotics (classical)

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3
Q

HALOPERIDOL

A

Typical antipsychotics (classical)

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4
Q

DROPERIDOL

A

Typical antipsychotics (classical)

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5
Q

Atypical antipsychotics (new generation)

A

D2 & D3 blockade: SULPIRIDE
5-HT2A / D2 blockade: CLOZAPINE, OLANZAPINE, QUETIAPINE, RISPERIDONE

Partial D2 & 5-HT1A agonist + 5-HT2A blockade: ARIPIPRAZOLE

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6
Q

SULPIRIDE

A 
Atypical antipsychotics (new generation)
D2 & D3 blockade
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7
Q

CLOZAPINE, OLANZAPINE, QUETIAPINE, RISPERIDONE

A 
Atypical antipsychotics (new generation)
5-HT2A / D2 blockade
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8
Q

ARIPIPRAZOLE

A 
Atypical antipsychotics (new generation)
Partial D2 & 5-HT1A agonist + 5-HT2A blockade
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9
Q

CLOZAPINE, QUETIAPINE

A 
Atypical antipsychotics (new generation)
5-HT2A / D2 blockade

High efficacy in refractory schizophrenias
concept of K-off or
dissociation rate

K-off preserves physiological function but hinders
pathological dopaminergic hyperactivity:
• Less extrapyramidal effects
• Less hyperprolactinemia
• Less phenomena of sensitization,
tolerance and positive D2 regulation
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10
Q

ARIPIPRAZOL

A

Atypical antipsychotics (new generation)

Partial D2 agonist
Competitive dualism:
• AGONIST in MESOCORTICAL pathway
• ANTAGONIST in MESOLIMBIC pathway
Partial 5-HT1A agonist
5-HT2A Antagonist
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11
Q

Typical antipyschotics (characteristics)

A

Typical antipsychotics:
•Effective on positive symptoms
•Poor effect on negative symptoms
•Mood swings and cognitive decline

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12
Q

Atypical antipyschotics (characteristics)

A 
•Do not produce catalepsy
•Less extrapyramidal effects
•Improve positive, negative, cognitive
& depressive symptoms
•Less hyperprolactinemia
•Less relapse risk
•Effective in refractory patients
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13
Q

Antipsychotic effect (in psychotic patients)

A

Independent of the sedative tranquilizing effect.
• Improve positive symptoms and a little the negative ones:
hallucinations, paranoid ideas, aggressiveness…
•Delayed effects
The efficacy in aggressive patients depends on this effect

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14
Q

Neuroleptic effect (tranquilizing)

A

In healthy people  SENSORIAL DEAFFERENTATION
Emotional quietude, psychomotor retardation & affective
indifference. Calmness. No sleep, but it looks like in a slumber.
Able to react to a strong stimulus.
• In psychotic patients
CATALEPSY at high doses
(motor immobility)

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15
Q

OTHER

A

Antiemetic effect
Bulbar dopaminergic antagonism and some anti-H1 effect
Respiratory depression by parenteral route
Neuroendocrine effects: Increase in prolactin secretion, decrease in
LH, FSH, GH and ADH, weight gain by:
• Inhibition of the tuberohypophyseal dopaminergic pathway
Vegetative effects (peripheral):
blockade of dopaminergic, α-adrenergic, cholinergic & histaminergic (H1)
receptors

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16
Q

Adverse effects

A 
Very frequent. Limiting the therapeutic compliance
6.1. Sedation
cholinergic & histaminergic (H1) blockade
mesolimbic pathway blockade
6.3. Endocrine:
•Hyperprolactinemia
•Dyslipidemias CLOZAPINE
•Weight gain CLOZAPINE + new antipsychotics
•Type II diabetes: CLOZAPINE + new antipsychotics
6.2. Vegetative
cholinergic, α-adrenergic blockade
D2 blockade: elongation of QT interval
6. Adverse effects
6.4. Hypersensitivity reactions:
•Photosensitivity
•Jaundice CHLORPROMAZINE
•Leucopenia, agranulocytosis CLOZAPINE
•Pigmentary retinopathy
6.5. Extrapyramidal motor effects
D2 blockade in nigrostriatal pathway
Acute dystonias, akathisia, Parkinson-like syndrome,
malign neuroleptic syndrome
* Chronic treatment:
Delayed dyskinesia: 20-40% patients taking typical
antipsychotics Disabling & irreversible
IMPORTANT:
Use the lowest therapeutic dose possible
Interactions:
Pharmacodynamic
Pharmacokinetic
17
Q

CLINCAL USES

A
  1. SCHIZOPHRENIA: Combine neuroleptics of different profile
    ▪ Gradual improvement in 6 weeks ▪ maximal response in 5-6 months
    ▪ Maintenance: 6-12 months
    OLANZAPINE, RISPERIDONE, HALOPERIDOL
  2. TOXIC PSYCHOSIS & POST-ALCOHOL SYNDROME
  3. DEMENTIA RISPERIDONE, HALOPERIDOL, (QUETIAPINE)
  4. MANIA & BIPOLAR DISORDRE RISPERIDONE, ARIPIPRAZOLE, OLANZAPINE,
    HALOPERIDOL, QUETIAPINE
  5. MAJOR DEPRESSION (+/- antidepressants) RISPERIDONE, QUETIAPINE
  6. NON-PSYCHIATRIC USES:
    TICS (Gilles de la Tourette’s syndrome) HALOPERIDOL
    NAUSEAS, VOMITS
    VERTIGO SULPIRIDE
    NEUROLEPTOANESTHESIA DROPERIDOL
    CHRONIC PAINS

DRUGS (22 decks)

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