MELISSA VAN DEVENTER

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MELISSA VAN DEVENTER

Blog #11

30 Apr 2021, 18:44 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

Aliphatic side-chain

Piperidine side-chain

Piperazine side-chain

Drug example

Chlorpromazine

Periciazine

Fluphenazine

Potency

Low potency

Low potency

High potency

Side effects

Severe sedation, little EPS, strong anti-cholinergic effects, strong alpha lytic effects, cardiotoxic

Severe sedation, strong anti-cholinergic effects, strong alpha lytic effects, cardiotoxic

More EPS, weaker anti-cholinergic effects, weaker alpha lytic effects, less sedation, less CVS effects

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

  • It blocks the D2 receptors mostly but it can also bind to muscarinic, alpha, histamine and serotonin receptors

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

  • The typical drugs work by blocking the D2 receptors found in the mesolimbic system
  • The atypical drugs block the 5-HT2A receptors more than the D2 receptors

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

  • The post-synaptic D2 receptors that are blocked by Benzamides

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

  • Butyrophenone derivatives (Haloperidol) due to the potent D2 blocking effects
  • Diphenylbutylpiperidines (Pimozide) due to potent D2 blocking effects

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

  • Due to the blockage of the a receptors