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PHARM 203 (Final) > Antidepressants (General) > Flashcards

Antidepressants (General) Flashcards

1
Q

Unipolar Depression

A

One direction of depressive symptoms

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2
Q

Bipolar Disorder

A

Depression alternating with mania

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3
Q

Depression Symptoms

A

Emotional:
- Sadness, Anxiety, Overwhelmed

Biological:
- Aches, Headaches, Sleep disturbance, Significant weight changes

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4
Q

Depression Pathophysiology (Monoamine Theory)

A

Depression is caused by deficient of monoamine transmitters, noradrenaline, and 5-HT

Mania is caused by excess

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5
Q

Evidence of Monoamine Theory

A

Tricyclic Antidepressants blocks NE and 5-HT reuptake
–> Increase NE and 5-HT in synapse
–> Increase mood

Reserpine inhibits NA and 5-HT storage
–> Decrease NA and 5-HT in body
–> Decrease body

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6
Q

Issues with Monoamine Theory

A

Inconsistent Result:
- Neurochemical effects of antidepressants is very rapid, however, antidepressant effects take weeks to form
–> What is happening in between giving monoamine and its antidepressive effects

  • Ketamine’s antidepressant effect works rapidly, however, it does not increase NA
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7
Q

Depression Neuroendocrine Mechanism
(Cortisol)

A

HPA Axis (Hypothalamus-Pituitary-Adrenocortical)

Stimulation of HPA (Caused by stress, illness, time of day, etc.)
- Hypothalamus releases CRH
- Anterior Pituitary releases ACTH
- Adrenal Glands release Cortisol (Stress Hormone)

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8
Q

Depression Neuroendocrine Mechanism
(Glutamate)

A

Stress enhances the excitotoxic effects of glutamate mediated by NMDA receptors
–> Expression of genes that promotes neural apoptosis

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9
Q

Depression Neuroendocrine Mechanism
(Neuron Loss)

A

Cortisol and Excitotoxic Glutamate promote Detrimental Gene Transcription Responses
–> Promotes Neural Apoptosis
–> Inhibits Neurogenesis

Promoting Depressive Symptoms

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10
Q

Depression Neuroendocrine Mechanism
(Neuron Gain)

A

NA, 5-HT, BDNF (Brain Derived Neurotrophic Factor) promote Beneficial Gene Transcription Responses
–> Promotes Neurogenesis
–> Inhibits Neural Apoptosis

Promoting Depressive Symptoms

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11
Q

Conventional Anti Depressants
(Inhibitors of Monoamine Uptake)

A
  • Selective Serotonin Reuptake Inhibitors (SSRIs)
  • Tricyclic Antidepressants (TCAs)
    –> NE and 5-HT Reuptake Inhibitors
  • Mixed 5-HT and NE Reuptake Inhibitors
    (SNRIs)
  • NE Dopamine Reuptake Inhibitors (NDRI)
  • St John’s Wort
    –> 5-HT and NE Reuptake Inhibitor
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12
Q

Conventional Anti Depressants
(Receptor Blocking Antidepressant)

A

Serotonin-2 Antagonists / Serotonin Reuptake Inhibitors (SARI)
–> Blocks 5HT-2

Noradrenergic/Specific Serotonergic Agent (NaSSA)

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13
Q

Monoamine Oxidase Inhibitors (MAOI)

A
  • Irreversible, non competitive, non selective inhibitors
    –> Inhibit MAO-A and MAO-B
    (Phenelzine, Tranylcypromine)
  • Reversible, MAO-A Selective Inhibitors
    (Moclobemide)
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14
Q

Rapid Acting Antidepressants (RAADs)

A

Non-Competitive NMDA Receptor Channel Blocker
- Ketamine

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15
Q

Effects of Antidepressants
(NE Reuptake Blockade)

A

Antidepressant Effect, Vasoconstrictor
Side Effect: Too much NE
- Causes tremors, tachycardia, and erectile problems
–> Avoid using with anything that increases heart rate

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16
Q

Effects of Antidepressants
(5-HT Reuptake Blockade)

A

Antidepressant, Anti-Anxiety, Anti-Panic, Anti-Obsessional

Side Effects: Affects other 5-HT Receptors
- Nausea, Dyspepsia, Headache, Sexual Side Effects

Potentiation of drugs with serotonin properties, caution regarding serotonin syndrome

17
Q

Effects of Antidepressants
(DA Reuptake Blockade)

A

Elevate Prolactin

Side Effects: Too much DA
- Aggravation of Psychosis

18
Q

Effects of Antidepressants
(5-HT1A Agonism)

A

Antidepressant, Anxiolytic, Anti Aggressive

19
Q

Effects of Antidepressants
(5-HT2A Blockade)

A

Anxiolytic, Antidepressant, Antipsychotic, Antimigraine, Improved Sleep

Side Effects:
- Hypotension, Ejaculatory Problems, Sedation, Weight Gain

20
Q

Effects of Antidepressants
(M1 Ach Blockade)

A

Dry mouth, blurred vision, urinary retention, constipation
Makes anticholinergic drugs stronger

21
Q

Effects of Antidepressants
(H1 Blockade)

A

Side Effects: Sedation, Postural Hypotension

22
Q

Effects of Antidepressants
(a1 Blockade)

A

Side Effects: Postural Hypotension, Dizziness, Reflex Tachycardia

23
Q

Effects of Antidepressants
(a2 Blockade)

A

CNS Effect: Possible decrease in depressive symptoms

24
Q

Adverse Effects of SSRIs

A

Enhanced effect on 5-HT Receptors
- Nausea, anorexia, insomnia, headache, nervousness, sexual dysfunction

Risk of Serotonin Syndrome

QT Interval Prolongation –> Citalopram

25
Q

Serotonin Modulator and Stimulator Benefits

A

Vortioxetine is more specific
Agonist: 5-HT1A and 5-HT1b
Antagonist: For other 5-HT

Due to being a specific agonist and its antagonist action –> Lower Side Effects
- Less sedation
- Less insomnia
- Less weight gain

26
Q

Serotonin-1A Agonist / Serotonin Reuptake Inhibitor (Mechanism)

A

Vilazodone

SSRI
Agonist for 5-HT1A

27
Q

Secondary Amines (Effects)

A

Greater NE Reuptake Inhibition than 5-HT effect
–> More NE Side Effects

28
Q

Tertiary Amines (Effects)

A

More 5-HT Reuptake Inhibition
–> More 5-HT Side Effects

29
Q

TCAs (Side Effects)

A

Affect Muscarinic, Histamine, and 5-HT Receptors

Overdose: Arrhythmia

  • Anticholinergic
    –> Dry mouth, blurred vision, constipation,
    urinary retention
  • Antihistamine
    –> Sedation
  • Antimuscarinic
30
Q

Venlafaxine

A

Non-Selective for 5-HT and NE uptake
- 5-HT Reuptake Inhibitor at low dose
- NE Reuptake Inhibitor at high dose

Similar to TCAs, lack major receptor blocking actions
–> Fewer Side Effects

31
Q

Bupropion

A

NDRI: NA and DA reuptake inhibitor

Helps in quitting smoking
Lowers seizure threshold
- Makes it easier to get seizure
–> Do not use with patients that are in risk of seizure

32
Q

Trazodone

A

SARI: Serotonin 2 Antagonist + Serotonin Reuptake Inhibitor

Blocks 5-HT2A and 5-HT2C
Blocks 5-HT Reuptake

Strong sedation effect:
- Should be taken at night

33
Q

Mirtazapine

A

NaSSA: Noradrenergic/Specific Serotonergic Agent

Blocks alpha 2 adrenoceptor and 5-HT2C receptors
–> Enhance NA and 5-HT release

Potent Antihistamine effect at H1

Also blocks 5-HT2A and 5-HT3 receptors
- Less sexual dysfunction and nausea side effects

No anticholinergic side effects

34
Q

Monoamine Oxidase (Different Types)

A

MAO-A (Main Antidepressant Target)
- Degrades 5-HT and NE
MAO-B
- Degrades phenylethylamine and dopamine

35
Q

Hypertensive Crisis

A

MAO in gut inactivates amines like tyramine
- Tyramine produces unwanted effects

If using a MAO inhibitor then there is no MAO to inactivate Tyramine
–> Can cause hypertensive crisis

Also avoid using OTC cough/cold agents that contain sympathomimetics

PHARM 203 (Final) (41 decks)

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