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Pharmacology > 23 Antipsychotic drugs > Flashcards

23 Antipsychotic drugs Flashcards

1
Q

23.01 FIRST-GENERATION ANTIPSYCHOTICS

Phenothiazines: chlorpromazine, fluphenazine, prochlorperazine - actions

A

antipsychotic
apathy and inertia
reduced aggression
antiemetic

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2
Q

23.01 FIRST-GENERATION ANTIPSYCHOTICS

Phenothiazines: chlorpromazine, fluphenazine, prochlorperazine - MOA

A

competitive antagonism of dopamine D2 receptors in the mesolimbic/mesocortical pathways
clinical benefits are delayed although receptor block is immediate, suggesting that more complex changes in neurotransmission occur

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3
Q

23.01 FIRST-GENERATION ANTIPSYCHOTICS

Phenothiazines: chlorpromazine, fluphenazine, prochlorperazine - abs/distrib/elim

A

given orally or by IM injection
half-life 16-32h
fluphenazine decanoate available as IM depot formulation

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4
Q

23.01 FIRST-GENERATION ANTIPSYCHOTICS

Phenothiazines: chlorpromazine, fluphenazine, prochlorperazine - clinical use

A

schizophrenia (less effective against negative symptoms) and other psychotic states
manic phase of bipolar disorder
Tourette’s syndrome
nausea and vomiting
aggression in children
persistent hiccups

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5
Q

23.01 FIRST-GENERATION ANTIPSYCHOTICS

Phenothiazines: chlorpromazine, fluphenazine, prochlorperazine - adverse effects

A

marked sedation
extrapyramidal symptoms (dystonias and parkinsonian symptoms) reduced by antimuscarinic action
endocrine effects (e.g. galactorrhoea, gynaecomastia, weight gain)
antimuscarinic effects (e.g. constipation, dry mouth)
hypotension (α-adrenoceptor antagonism)
rare, but serious, neuroleptic malignant syndrome
hypersensitivity reactions
agranulocytosis
hepatotoxicity

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6
Q

23.02 FIRST-GENERATION ANTIPSYCHOTICS

Butyrophenone: haloperidol - actions

A

antipsychotic
apathy
reduced aggression
antiemetic

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7
Q

23.02 FIRST-GENERATION ANTIPSYCHOTICS

Butyrophenone: haloperidol - MOA

A

competitive antagonism of dopamine D2 receptors in the mesolimbic/mesocortical pathways
clinical benefits are delayed although receptor block is immediate, suggesting that more complex changes in neurotransmission occur
higher potency compared to chlorpromazine

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8
Q

23.02 FIRST-GENERATION ANTIPSYCHOTICS

Butyrophenone: haloperidol - abs/distrib/elim

A

given orally or IM (also IM depot)
half-life 12-36h

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9
Q

23.02 FIRST-GENERATION ANTIPSYCHOTICS

Butyrophenone: haloperidol - clinical use

A

schizophrenia (less effective against negative symptoms) and other psychotic states
mania
Tourette’s syndrome
nausea and vomiting
aggressive behaviour
persistent hiccups

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10
Q

23.02 FIRST-GENERATION ANTIPSYCHOTICS

Butyrophenone: haloperidol - adverse effects

A

marked extrapyramidal symptoms
hyperprolactinaemia
little sedative, hypotensive or antimuscarinic actions neuroleptic malignant syndrome

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11
Q

23.02 FIRST-GENERATION ANTIPSYCHOTICS

Butyrophenone: haloperidol - special notes

A

contraindicated in patients with Parkinson’s disease

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12
Q

23.03 FIRST-GENERATION ANTIPSYCHOTICS

Thioxanthenes: flupentixol, zuclopentixol - actions

A

antipsychotic
antidepressant (tricyclic-like) activity

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13
Q

23.03 FIRST-GENERATION ANTIPSYCHOTICS

Thioxanthenes: flupentixol, zuclopentixol - MOA

A

competitive antagonism of dopamine D2 receptors in the mesolimbic/mesocortical pathways
clinical benefits are delayed although receptor block is immediate, suggesting that more complex changes in neurotransmission occur

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14
Q

23.03 FIRST-GENERATION ANTIPSYCHOTICS

Thioxanthenes: flupentixol, zuclopentixol - abs/distrib/elim

A

effective orally but most often given by IM depot
half-life 19-39h

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15
Q

23.03 FIRST-GENERATION ANTIPSYCHOTICS

Thioxanthenes: flupentixol, zuclopentixol - clinical use

A

schizophrenia and other psychotic states
bipolar disorder
depression

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16
Q

23.03 FIRST-GENERATION ANTIPSYCHOTICS

Thioxanthenes: flupentixol, zuclopentixol - adverse effects

A

extrapyramidal symptoms
hyperprolactinaemia
neuroleptic malignant syndrome

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17
Q

23.04 SECOND-GENERATION ANTIPSYCHOTICS

Clozapine, olanzapine - actions

A

antipsychotic
effective against positive and negative symptoms

18
Q

23.04 SECOND-GENERATION ANTIPSYCHOTICS

Clozapine, olanzapine - MOA

A

MOA less well established than for typical agents
action on 5-HT2A receptors may be important
antagonist action at 5-HT2, muscarinic, H1 histamine receptors and α1 adrenoceptors
higher affinity for D4 than other dopamine receptors

19
Q

23.04 SECOND-GENERATION ANTIPSYCHOTICS

Clozapine, olanzapine - abs/distrib/elim

A

orally active
half-life 12h

20
Q

23.04 SECOND-GENERATION ANTIPSYCHOTICS

Clozapine, olanzapine - clinical use

A

schizophrenia
because of haematological toxicity, clozapine is used mainly in patients resistant to other drugs, for whom it is very effective
olanzapine is also used for manic episodes and bipolar disorder

21
Q

23.04 SECOND-GENERATION ANTIPSYCHOTICS

Clozapine, olanzapine - adverse effects

A

little extrapyramidal symptoms (reduced D2 antagonism coupled with antimuscarinic action)
antimuscarinic actions (e.g. constipation)
agranulocytosis (not with olanzapine) - blood testing needed
sedation
epileptic seizures
weight gain (more than with other antipsychotics) hyperglycaemia

22
Q

23.05 SECOND-GENERATION ANTIPSYCHOTICS

Risperidone - actions

A

antipsychotic
effective against positive and negative symptoms of schizophrenia

23
Q

23.05 SECOND-GENERATION ANTIPSYCHOTICS

Risperidone - MOA

A

potent antagonist of D2 and 5-HT2A receptors and α1 adrenoceptors
as for other atypical agents, a combination of D2 and 5-HT2A antagonism may be important in modifying activity in the mesolimbic/mesocortical pathways

24
Q

23.05 SECOND-GENERATION ANTIPSYCHOTICS

Risperidone - abs/distrib/elim

A

given orally or by IM depot
hepatic P450 metabolism
half-life 3-20h
active metabolite is longer acting

25
Q

23.05 SECOND-GENERATION ANTIPSYCHOTICS

Risperidone - clinical use

A

schizophrenia and other psychotic states
manic phase of bipolar disorder

26
Q

23.05 SECOND-GENERATION ANTIPSYCHOTICS

Risperidone - adverse effects

A

extrapyramidal symptoms (more than with other atypicals)
insomnia and sedation
anxiety
hyperprolactinaemia
weight gain
hypotension

27
Q

23.06 SECOND-GENERATION ANTIPSYCHOTICS

Quetiapine - actions

A

antipsychotic
effective against positive and negative symptoms

28
Q

23.06 SECOND-GENERATION ANTIPSYCHOTICS

Quetiapine - MOA

A

competitive antagonism of dopamine D2 and 5-HT2A receptors in the mesolimbic/mesocortical pathways
antagonism of H1 histamine receptors may underlie sedative action

29
Q

23.06 SECOND-GENERATION ANTIPSYCHOTICS

Quetiapine - abs/distrib/elim

A

given orally
short (6h) half-life

30
Q

23.06 SECOND-GENERATION ANTIPSYCHOTICS

Quetiapine - clinical use

A

schizophrenia and other psychotic states
bipolar disorder

31
Q

23.06 SECOND-GENERATION ANTIPSYCHOTICS

Quetiapine - adverse effects

A

minor extrapyramidal symptoms
sedation
hyperprolactinaemia
weight gain
postural hypotension
constipation, dry mouth (antimuscarinic actions)
rarely, neuroleptic malignant syndrome

32
Q

23.07 SECOND-GENERATION ANTIPSYCHOTICS

Aripiprazole - actions

A

antipsychotic
effective against positive and negative symptoms

33
Q

23.07 SECOND-GENERATION ANTIPSYCHOTICS

Aripiprazole - MOA

A

modification of dopaminergic transmission in the mesolimbic/mesocortical pathways
aripiprazole binds strongly to dopamine D2 receptors but has partial agonist activity, which may explain its low incidence of extrapyramidal symptoms
5-HT2A antagonism is probably important

34
Q

23.07 SECOND-GENERATION ANTIPSYCHOTICS

Aripiprazole - abs/distrib/elim

A

given orally
long (75h) half-life

35
Q

23.07 SECOND-GENERATION ANTIPSYCHOTICS

Aripiprazole - clinical use

A

schizophrenia and other psychotic states
manic phase of bipolar disorder

36
Q

23.07 SECOND-GENERATION ANTIPSYCHOTICS

Aripiprazole - adverse effects

A

fewer side effects than many other antipsychotics, e.g. minor extrapyramidal symptoms (some akathisia), less weight gain, less antimuscarinic, less prolactin secretion
some hypotension and nausea and vomiting

37
Q

23.08 SECOND-GENERATION ANTIPSYCHOTICS

Amisulpride, sulpiride - actions

A

antipsychotic
effective against positive and negative symptoms of schizophrenia

38
Q

23.08 SECOND-GENERATION ANTIPSYCHOTICS

Amisulpride, sulpiride - MOA

A

dopamine D2 and D3 receptor antagonists
preferential action on dopamine autoreceptors may explain the lower incidence of EPS and effectiveness against −ve symptoms
low affinity for 5-HT, muscarinic, histamine and α1 adrenergic receptors

39
Q

23.08 SECOND-GENERATION ANTIPSYCHOTICS

Amisulpride, sulpiride - abs/distrib/elim

A

mostly excreted unchanged in kidney
half-life 12h

40
Q

23.08 SECOND-GENERATION ANTIPSYCHOTICS

Amisulpride, sulpiride - clinical use

A

schizophrenia

41
Q

23.08 SECOND-GENERATION ANTIPSYCHOTICS

Amisulpride, sulpiride - adverse effects

A

hyperprolactinaemia
insomnia
anxiety
weight gain
constipation and dry mouth

Pharmacology (34 decks)

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