IZANNE BIELDT

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Blog #12

20 May 2021, 17:40 Publicly Viewable

  1. Using your textbooks, draw up a classification of the drugs that are used as antidepressants.

Classification

Drug

Tricyclic antidepressants (TCA)

Tertiary Amine

  • Amitriptyline
  • Imipramine
  • Trimipramine
  • Chlorprimipramine
  • Dothiepine
  • Butriptyline

Secondary Amine

  • Nortiptyline
  • Desimipramine
  • Lofepramine

Monoamine oxidase inhibitors (MAOI’s)

Tranylcyclopromine: Non selective MOAI

Moclobemide: Selective MOA-A inhibitor  

Selective 5HT reuptake inhibitors (SSRI)

Fluoxetine

Paroxetine

Fluvoxamine

Sertraline

Citalopram

Escitalopram

Serotonin and noradrenalin reuptake inhibitors (SNRI’s)

Venflaxine

Duloxetine

Selective noradrenaline reuptake inhibitors (NAR’s)

Reboxetine

Tetracylcic and unicyclic AD’s

Mianserin (Tetracyclic)

Mirtaxepine (Tetracyclic)

Bupropion (Unicyclic)

5-HT2 Receptor modulators

Trazodone

Vortioxetine

Circadian rhythym regulators

Aglomelatine

  1. What do the existing drugs all have in common regarding their mechanisms of action?

Multipotent actions on numerous monoamine receptors which leads to the non-specific increase of 5-HT or NA

  1. How long does it take for the antidepressive effects of these drugs to appear? What is the reason for this?

The clinical response can take up to 3-5 weeks. This long period can be explained by the effects of the antidepressant drug on the neurotrphic factors. It can take two weeks or longer for the synthesis of neurotrophic factors to take place.

  1. How do the TADs and the selective serotonin reuptake inhibitors (SSRI’s) differ in respect of:

*Look up in textbook and add

TAD’s

SSRI’s

Efficacy

Require up titration to minimum effective dosage

Can immediately start with full dosage administration

Side effects

  • Sedation
  • Tremore and insomnia (Sympathomimetic effects)
  • Visual disturbances, Dry mouth, Constipation, Urinary retention, confusion (Anti-cholinergic effects)
  • Cardio-vascular: Orthostatic hypotention. Dysrhthmia
  • Convulsions
  • Metabolic-endocrine: Weigh decrease, Sexual disturbances
  • Psychosis and can precipitate mania
  • Anxiety
  • Sexual dysfunction
  • Insomnia
  • Headache
  • GIT distubrances
  • Decreases Libido
  • Extra-pyramidial side effects
  • Withdrawal syndrome

Safety

Acute overdose is extremely dangerous and can lead to: coma, convulsions and cardio-toxicity

Safer to use, fewer side effects

  1. What is the action of mirtazapine?

Tetracyclic Antidepressant. Mirtrazepine primarily blocks a2 receptors which causes an increase in NA(autoreceptors) and 5-HT(heterorecpetors) release.

It also blcoks  5-HT2A (Anti-depressive effects)  and blocks 5-HT3 (anxiolytic and decrease nausea).

Additionally it also blocks H1 receptors which leads to sedation and weight gain, and it blocks a1 receptors which can lead to postural hypotension.

  1. What is the action of venlafaxine?

Serotonin and noradrenaline reuptake inhibitor. Blocks both 5-HT and NA re-uptake, but has a higher affinity for 5-HT than NA

  1. What is the action of agomelatine?

Circadian rhythm regulator. MT 1 and MT 2 agonist and 5-HT2c antagonist. MT 1 and MT 2 agonism helps in regulation of circadian rhythyms and improves sleep. 5-HT2C antagonism improves sleep through regulation of circadian rhythms and also provides antidepressant action. 5-HT2C antagonism leads to disinhibition of DA and NA release in the frontal cortex, which leads to an increase in Dopamine and NA release.

Brand, L. 2021. Anti-depressants. Study Unit 10. [PowerPoint Presentation]. Study Unit 10, FKLG 312. Potchefstroom, NWU.