23 Antipsychotic drugs Flashcards by Emma :)

Q

23.01 FIRST-GENERATION ANTIPSYCHOTICS

Phenothiazines: chlorpromazine, fluphenazine, prochlorperazine - actions

A

antipsychotic
apathy and inertia
reduced aggression
antiemetic

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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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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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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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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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Q

23.02 FIRST-GENERATION ANTIPSYCHOTICS

Butyrophenone: haloperidol - actions

A

antipsychotic
apathy
reduced aggression
antiemetic

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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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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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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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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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Q

23.02 FIRST-GENERATION ANTIPSYCHOTICS

Butyrophenone: haloperidol - special notes

A

contraindicated in patients with Parkinson’s disease

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Q

23.03 FIRST-GENERATION ANTIPSYCHOTICS

Thioxanthenes: flupentixol, zuclopentixol - actions

A

antipsychotic
antidepressant (tricyclic-like) activity

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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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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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Q

23.03 FIRST-GENERATION ANTIPSYCHOTICS

Thioxanthenes: flupentixol, zuclopentixol - clinical use

A

schizophrenia and other psychotic states
bipolar disorder
depression

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Q

23.03 FIRST-GENERATION ANTIPSYCHOTICS

Thioxanthenes: flupentixol, zuclopentixol - adverse effects

A

extrapyramidal symptoms
hyperprolactinaemia
neuroleptic malignant syndrome

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Q

23.04 SECOND-GENERATION ANTIPSYCHOTICS

Clozapine, olanzapine - actions

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A

antipsychotic
effective against positive and negative symptoms

Q

23.04 SECOND-GENERATION ANTIPSYCHOTICS

Clozapine, olanzapine - MOA

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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

Q

23.04 SECOND-GENERATION ANTIPSYCHOTICS

Clozapine, olanzapine - abs/distrib/elim

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A

orally active
half-life 12h

Q

23.04 SECOND-GENERATION ANTIPSYCHOTICS

Clozapine, olanzapine - clinical use

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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

Q

23.04 SECOND-GENERATION ANTIPSYCHOTICS

Clozapine, olanzapine - adverse effects

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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

Q

23.05 SECOND-GENERATION ANTIPSYCHOTICS

Risperidone - actions

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A

antipsychotic
effective against positive and negative symptoms of schizophrenia

Q

23.05 SECOND-GENERATION ANTIPSYCHOTICS

Risperidone - MOA

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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

Q

23.05 SECOND-GENERATION ANTIPSYCHOTICS

Risperidone - abs/distrib/elim

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A

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

23.05 SECOND-GENERATION ANTIPSYCHOTICS Risperidone - clinical use

schizophrenia and other psychotic states manic phase of bipolar disorder

23.05 SECOND-GENERATION ANTIPSYCHOTICS Risperidone - adverse effects

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

23.06 SECOND-GENERATION ANTIPSYCHOTICS Quetiapine - actions

antipsychotic effective against positive and negative symptoms

23.06 SECOND-GENERATION ANTIPSYCHOTICS Quetiapine - MOA

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

23.06 SECOND-GENERATION ANTIPSYCHOTICS Quetiapine - abs/distrib/elim

given orally short (6h) half-life

23.06 SECOND-GENERATION ANTIPSYCHOTICS Quetiapine - clinical use

schizophrenia and other psychotic states bipolar disorder

23.06 SECOND-GENERATION ANTIPSYCHOTICS Quetiapine - adverse effects

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

23.07 SECOND-GENERATION ANTIPSYCHOTICS Aripiprazole - actions

antipsychotic effective against positive and negative symptoms

23.07 SECOND-GENERATION ANTIPSYCHOTICS Aripiprazole - MOA

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

23.07 SECOND-GENERATION ANTIPSYCHOTICS Aripiprazole - abs/distrib/elim

given orally long (75h) half-life

23.07 SECOND-GENERATION ANTIPSYCHOTICS Aripiprazole - clinical use

schizophrenia and other psychotic states manic phase of bipolar disorder

23.07 SECOND-GENERATION ANTIPSYCHOTICS Aripiprazole - adverse effects

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

23.08 SECOND-GENERATION ANTIPSYCHOTICS Amisulpride, sulpiride - actions

antipsychotic effective against positive and negative symptoms of schizophrenia

23.08 SECOND-GENERATION ANTIPSYCHOTICS Amisulpride, sulpiride - MOA

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

23.08 SECOND-GENERATION ANTIPSYCHOTICS Amisulpride, sulpiride - abs/distrib/elim

mostly excreted unchanged in kidney half-life 12h

23.08 SECOND-GENERATION ANTIPSYCHOTICS Amisulpride, sulpiride - clinical use

schizophrenia

23.08 SECOND-GENERATION ANTIPSYCHOTICS Amisulpride, sulpiride - adverse effects

hyperprolactinaemia insomnia anxiety weight gain constipation and dry mouth