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Pharmacology > Pharmacology of depression > Flashcards

Pharmacology of depression Flashcards

1
Q

What are the core drugs used to treat depression?

A

Sertraline
Citalopram
Fluoxetine
Venlafaxine
Mirtazapine

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2
Q

What is the primary mechanism of action of Sertaline?

A

Inhibition of serotonin reuptake results in an accumulation of serotonin. Serotonin in the central nervous system plays a role in the regulation of mood, personality, and wakefulness.

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3
Q

What is the drug target of Sertraline?

A

Serotonin transporter

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4
Q

What are the main side effects of Sertraline?

A

GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia

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5
Q

What affect can Sertraline have on dopamine levels?

A

Mild inhibition of dopamine transporter

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6
Q

Why is it important to monitor the dosage of Sertraline?

A

Must be gradually decreased on discontinuation. Partial inhibition of CYP2D6 at high doses (150 mg)- CYP2D6 inhibitors can decrease efficacy of many drugs as the CYP2D6 enzyme is involved in the metabolism of many drugs

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7
Q

What is the primary mechanism of action of Citalopram?

A

Inhibition of serotonin reuptake results in an accumulation of serotonin. Serotonin in the central nervous system plays a role in the regulation of mood, personality, and wakefulness.

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8
Q

What is the drug target of Citalopram?

A

Serotonin transporter

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9
Q

What are the main side effects of Citalopram?

A

GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia

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10
Q

What affect can Citalopram have on other parts of the body?

A

Mild antagonism of muscarinic and histamine (H1) receptors

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11
Q

Why does the dose of Citalopram need to be monitored?

A

Must be gradually decreased on discontinuation. Metabolized by CYP2C19.

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12
Q

What is the primary mechanism of action of Fluoxetine?

A

Inhibition of serotonin reuptake results in an accumulation of serotonin. Serotonin in the central nervous system plays a role in the regulation of mood, personality, and wakefulness.

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13
Q

What is the drug target of Fluoxetine

A

Serotonin transporter

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14
Q

What are the main side effects of Fluoxetine

A

GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia

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15
Q

What affect can Fluoxetine have on the rest of the body?

A

Mild antagonism of 5HT2A and 5HT2C receptors
Complete inhibition of CYP2D6 and significant inhibition of CYP2C19 (caution with warfarin).

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16
Q

What is the primary mechanism of action of Venlafaxine

A

Venlafaxine is a more potent inhibitor of serotonin reuptake than norepinephrine reuptake.
Noradrenaline in the central nervous system is implicated in the regulation of emotions and cognition.

17
Q

What is the drug target of Venlafaxine?

A

Serotonin transporter
Noradrenaline transporter

18
Q

What are the main side effects of Venlafaxine

A

GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia, hypertension (at higher doses)

19
Q

What is important to consider during the discontinuation of Venlafaxine?

A

Must be gradually decreased on discontinuation- wash out the drug before prescribing a new one to avoid drug-drug interactions (v. dangerous)

20
Q

What is the primary mechanism of action for Mirtazapine?

A

Antagonises central presynaptic alpha-2-adrenergic receptors, which causes an increased release of serotonin and norepinephrine.
Antagonises central 5HT2 receptors, which leaves 5HT1 receptors unopposed causing anti-depressant effects.

21
Q

What are the drug targets of Mirtazapine?

A

Alpha-2 receptor
5-HT2 receptor

22
Q

What are the main side effects of Mirtazapine

A

Weight gain, sedation,
Less common: May exacerbate REM sleep behaviour disorder
Low probability of sexual dysfunction

23
Q

Why is it important that many of the anti-depressant drugs are gradually decreased on discontinuation

A
  1. Have to be decreased/ discontinued before prescribing a new drugs: need to do a wash out to avoid drug- drug interference (can be v. dangerous)
  2. Gradually: body becomes used to/ dependent on the old drug/ effects of the old- needs to be washed out to avoid side effects
24
Q

What are “the seven steps” for prescribing drugs to patients?

A
  1. Identify the patient’s problem
  2. Specify the therapeutic objective
  3. Select a drug on the basis of comparative efficacy, safety, cost and suitability
  4. Discuss choice of medication with patient (and carer) and make a shared decision about treatment
  5. Write a correct prescription
  6. Counsel the patient on appropriate use of the medicine
  7. Make appropriate arrangements for follow up (Monitor/stop the treatment)
25
Q

What is used to screen for depression in primary care?

A

the Patient health Questionnaire 9 (PHQ-9)= 9 step questionnaire

26
Q

Describe the mechanism of action of SSRIs treatment?

A

Selective serotonin reuptake inhibitors (SSRIs)

  • Serotonin is a neurotransmitter thought to have a good influence on mood, emotion and sleep.
  • After carrying a message, serotonin is usually reabsorbed by the nerve cells (known as “reuptake”). - - SSRIs work by blocking (“inhibiting”) reuptake, meaning more serotonin is available to pass further messages between nearby nerve cells
  • A rise in serotonin levels can improve symptoms and make people more responsive to other types of treatment, such as CBT.
27
Q

When should you avoid prescribing Citalopram?

A

Both erythromycin and citalopram prolong the QT interval. Most manufacturers advise the use of two or more durgs that are associated with QT prolongation. (excessive QT prolongation carries a risk of sudden cardiac death (SCD) due to polymorphic tachycardia)

28
Q

Why do the therapeutic effects of SSRIs plateau eventually?

A
  • Finite no. of serotonin receptors
  • Receptors become fully saturated; effects decrease
29
Q

What are ALL the drug targets of Mirtazapine (not just the anti-depressant ones)

A
  1. Histamine H1 receptor (for sedation)
  2. Alpha-2 receptor (Anti-depressant effect)
  3. 5HT2 receptor (Anti-depressant effect)
  4. 5HT3 receptor (Anti-emetic effect)
30
Q

What are the effects of having so many drug targets like Mirtazapine

A
  1. Not v. selective- in this case it is advantageous as all 4 effects contribute to help reduce depressive symptoms
31
Q

Mirtazapine has so many drug target- how do we know which is being targetted?

A

No clear indication but Histamine H1 receptor has the highest affinity, and 5HT3 has the lowest affinity

Pharmacology (7 decks)

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