C OLIVIER

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Blog #11

3 May 2021, 13:12 Publicly Viewable

Name an example of each of the three phenothiazine sub-families and state how they differ from one another in terms of potency and side effects.

SUB-FAMILY EXAMPLE POTENCY SIDE EFFECTS
Aliphatic side chain Chlorpromazine Low potency

Little EPS

Severe sedation

Strong anti-cholinergic effects

Strong alpha-lytic effects (postural hypotension)

Cardiotoxic

Piperidine side chain Periciazine Low potency

Little EPS

Severe sedation

Strong anti-cholinergic effects

Strong alpha-lytic effects (postural hypotension)

Cardiotoxic

Piperazine side chain Fluphenazine High potency

More EPS

Weaker anti-cholinergic effects

Weaker alpha-lytic

Less sedation

Less Cardiovascular side effects

Which receptors in particular are blocked by the typical antipsychotic drugs?

Block Mesolimbic D2 receptors

How does the mechanism of action of the atypical drugs differ from that of the typical drugs?

  • Atypical: Blocks both serotonin and dopamine receptors in the limbic system, thereby decreasing the response of postsynaptic neuron to dopamine and serotonin excitation. These drugs also inhibits H1, cholinergic and alpha-adrenergic receptors, although the activity of atypical AP at these off target receptors are much less than that of the typical APs.
  • Typical: Block post-synaptic D2 receptors in the limbic system, thereby decreasing the response of the post-synaptic neuron to DA excitation. These drugs also inhibit H1, cholinergic and alpha-adrenergic receptors. Thus, they are multi-potent competitive antagonists.

Which of the receptors blocked by the older drugs reduce the risk of extrapyramidal side effects?

D3 receptors

Which of the older drugs have a high incidence of extrapyramidal side effects? What is the reason for this?

Haloperidol

This drug is a potent D2 blocker, which increases the prevalence of EPS

Because of which receptor(s) blockade do the aliphatic group of drugs have a high incidence of autonomic side effects?

Cholinergic receptors