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pharmacology Neuro > antidepressants > Flashcards

antidepressants Flashcards

1
Q

What is the process of the typical antidepressants?

A
  1. Monoamine Oxidase Inhibitors (MAOI)
  2. Tricyclic Antidepressants (TCA)
  3. Selective Serotonin Reuptake Inhibitors (SSRI)
  4. Selective Noradrenaline Reuptake Inhibitors (NRI)
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2
Q

Give examples of monoamine oxidase inhibitors (MAOIs)

A

Iproniazid

Moclobemide

Phenelzine

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3
Q

What is the mechanism of the MAOIs Iproniazid, Moclobemide, and phenelzine

A
  1. Inhibit breakdown of monoamines
  2. Irreversible and reversible inhibitors of MAO-A and /or B
  3. MAO found in all tissues including GI tract
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4
Q

What are the side effects of the MAOIs Iproniazid, Moclobemide, and phenelzine

A
  1. M1 → atropine like symptoms dry mouth and blurred vision
  2. Alpha1 → dizzy light headiness
  3. H1 → sedation
  4. 5-HT2
  5. Cheese reaction
  6. Drug interactions
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5
Q

Describe the cheese reaction

A
  1. MAO (GIT and liver) plays an important role in metabolism of ingested substances
  2. Patients taking IRREVERSIBLE MAOI cannot metabolise ingested amines such as tyramine leading to high levels in the blood.
  3. Tyramine displaces noradrenaline from its terminals causing acute hypertension which can cause intracranial haemorrhage.
  4. Occurs with irreversible inhibitors such as phenylzine.
  5. This is not seen with reversible MAOI such as moclobemide.
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6
Q

Describe some of the drug interactions with MAOIs

A

Drugs such as amphetamine will also cause the cheese type reaction in people taking MAOIs.

Pethidine (opioid) will cause hyperpurexia (elevation in body temperature) with restlessness, coma and hypotension with MAOIs

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7
Q

Give examples of Tricyclic Antidepressants (TCA)

A

Imipramine
Amitriptyline
Clomipramine
Desipramine

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8
Q

What is the mechanism of the Tricyclic Antidepressants (TCA)

A
  1. Block reuptake of monoamines (mainly NA and 5-HT, relative selectivity varies)
  2. Some block alpha2-AR
  3. Many have active metabolites
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9
Q

what are the side effects of the Tricyclic Antidepressants (TCA)

A 
Histamine antagonist
Muscarinic actions
Alpha1 adrenergic
5-HT2 effects
cardiotoxic - cause tachycardia, arrythmias and hypotension
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10
Q

Give examples of Selective Reuptake Inhibitors (SSRI + SNRI) and the

A

Fluoxetine - 5HT specific re-uptake receptor
paroxetine - 5HT specific re-uptake receptor
citalopram - 5HT specific re-uptake receptor

Venlafaxine -seretonin-noradrenaline re-uptake inhibitor (SNRI)

Reboxetine - NA specific re-uptake inhibitor

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11
Q

What is the mechanism of action of Selective Reuptake Inhibitors (SSRI + SNRI)

A

Block the re-uptake of 5-HT or noradrenaline or both NA and 5-HT

Lack cholinergic side-effects

No food interaction

Reduced drug interactions

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12
Q

What are the 5HT side effects of Selective Reuptake Inhibitors

A 
Nausea
Anorexia
Insomnia
Sexual dysfunction
5-HT syndrome (similar to ‘Ecstasy’ OD)
Increase suicide risk in adolescents
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13
Q

What are the noradrenaline side effects of Selective Reuptake Inhibitors

A 
Difficulty sleeping (insomnia)
Constipation
Sweating
Sympathetic effects – tachycardia
Anxiety, irritability, aggression
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14
Q

Give some examples of atypical antidepressant drugs

A 
Venlafaxine
Trazodone
Nefazedone
Mirtazapine
Agomelatine
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15
Q

What is the mechanism of action of Venlafaxine

A

serotonin-noradrenaline re-uptake inhibitor (SNRI)

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16
Q

When is Venlafaxine used

A

severely depressed
retarded
hypersomnic

17
Q

what is the mechanism of action of Trazodone

A

Selective 5HT re-uptake inhibitor

5HT-2 antagonist

18
Q

what is the mechanism of action of Nefazedone

A

Selective NA re-uptake inhibitor

5HT-2 antagonist

19
Q

What dies 5HT-2 antagonism do

A 
Reduces anxiety
Improved slow wave sleep
Reduce sexual dysfunction
Sedation
Improves side effects associated with serotonin
20
Q

what is the mechanism of action of Mirtazapine

A

Noradranaline receptor antagonist

5HT receptor antagonist

21
Q

what is the mechanism of action of Agomelatine

A

melatonin agonist

5HT-2 antagonist

22
Q

Treatment of Bipolar:

A

Acute:

  1. Lithium or Carbamazepine,
  2. 2nd line – Valporate
23
Q

Treatment to prevent bipolar disorder (prophylaxis)

A

Prophylaxis:

  1. 1st line lithium and olanzapine
  2. 2nd line Carbamazepine

pharmacology Neuro (14 decks)

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