Anxiolytics

Anxiety drugs: the name, MOA and side effects.

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SSRI: MOA?
Inhibit serotonin transporter, increase serotonin in synaptic cleft, more receptor activation = serotonergic neurones inhibit amygdala, thalamus, striatum and cortex.
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SSRI: pros and cons?
Tolerated well and used as long term therapy, but clinical effect takes weeks - months (maybe neurogenesis), sexual dysfunction, weight gain, initial increase in anxiety.
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SSRI: examples
Prozac (Fluoxetine)
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Why do side effects of SSRi happen (2)?
Stimulation of wrong serotonin receptor or stimulation of correct receptor but in wrong part of brain.
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NRI and SNRI: MOA?
Chronic use leads to down regulation of alpha 1 and beta 1 receptors therefore inhibiting over activation of noradrenaline neurones.
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Examples of NRI and SNRI?
Reboxetine and Venlafaxine.
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NRI and SNRI: pros and cons?
Hepatotoxicity of duloxetine, initial increase in anxiety, take weeks - months for clinical effects, SNRI inhibit both serotonergic and noradrenergic neurones.
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Benzodiazepines: MOA?
Enhance inhibitory GABAergic interneurone activity in amygdala and pre frontal cortex.
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Benzodiazepines: examples?
Lorazepam
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Benzodiazepines: pros and cons?
Rapid onset so better for shorter term therapy, low risk of abuse, can be used with SSRI, but side effects: cognitive impairement and ataxia
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Tricyclic antidepressants: MOA?
Inhibit serotonin and noradrenaline reuptake, also block muscarinic AchR, H1R and a1R.
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Tricyclic antidepressants: examples
Imipramine
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Tricyclic antidepressants: pros and cons?
Imipramine effective for GAD, but anticholinergic, antihistaminic and antinoraadrenergic side effects, less well tolerated and more toxic in overdose than SSRI
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Pregabalin: MOA?
Binds to alpha-2-delta subunit of P/Q type voltage gated calcium channel = negative allosteric modulation = reduce calcium influx, reduce vesicle-membrane fusion, reduce neurotransmitter release
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SSRI: pros and cons?

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Tolerated well and used as long term therapy, but clinical effect takes weeks - months (maybe neurogenesis), sexual dysfunction, weight gain, initial increase in anxiety.

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SSRI: examples

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Card 4

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Why do side effects of SSRi happen (2)?

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Card 5

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NRI and SNRI: MOA?

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